Month: September 2022

Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. 10111-08-7, formula is C4H4N2O, Name is 1H-Imidazole-2-carbaldehyde. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents. Synthetic Route of 10111-08-7.

Eckhardt, Andre K. research published 《 Spectroscopic evidence for 1,2-diiminoethane – a key intermediate in imidazole synthesis》, the research content is summarized as follows. Simple imines and diimines are common building blocks in organic synthesis, but the compound class is spectroscopically not well characterized. Herein we report the formation of the simplest diimine, namely 1,2-diiminoethane, as well as spectroscopic characterization by cryogenic matrix isolation IR and UV/Vis spectroscopy. Three conformers of 1,2-diiminoethane form after UV irradiation of 1,2-diazidoethane by N₂ extrusion at 3 K in solid argon and can be photochem. interconverted. In a matrix isolation pyrolysis experiment at 600°C with 1,2-diazidoethane as the starting material we observe hydrogen cyanide and formaldimine as the main decomposition products. All exptl. findings are supported by deuterium labeling experiments and B3LYP/6-311++G(2d,2p) calculations Irradiation of 1,2-diazidoethane in aqueous solution leads to the formation of imidazoles as indicated by NMR spectroscopy and GC-MS anal. Our results underline the key role of diimines as building blocks in N-heterocyclic chem.

10111-08-7, 1H-Imidazole-2-carbaldehyde, also known as 1H-Imidazole-2-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
1H-Imidazole-2-carboxaldehyde is a novel PTP1b inhibitor with potential application to treat type 2 diabetes.
1H-Imidazole-2-carboxaldehyde is a broad-spectrum antimicrobial that has been shown to inhibit the growth of bacteria by interfering with protein synthesis. It binds to the cytosolic protein and receptor molecule, which are involved in the activation of bacterial enzymes. Imidazole-2-carboxaldehyde reacts with anhydrous sodium and copper complex to produce hydrogen bonds, which prevent the formation of the nitrogen atoms necessary for cellular processes. This chemical also has biological properties such as glyoxal, which inhibits bacterial growth by reacting with amino groups on proteins., Synthetic Route of 10111-08-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen. Application In Synthesis of 60-56-0.

D’Urso, Ottavio;Drago, Filippo research published 《 Pharmacological significance of extra-oral taste receptors》, the research content is summarized as follows. A review. It has recently been shown that taste receptors, in addition to being present in the oral cavity, exist in various extra-oral organs and tissues such as the thyroid, lungs, skin, stomach, intestines, and pancreas. Although their physiol. function is not yet fully understood, it appears that they can help regulate the body’s homeostasis and provide an addnl. defense function against pathogens. Since the vast majority of drugs are bitter, the greatest pharmacol. interest is in the bitter taste receptors. In this review, we describe how bitter taste 2 receptors (TAS2Rs) induce bronchodilation and mucociliary clearance in the airways, muscle relaxation in various tissues, inhibition of TSH (TSH) in thyrocytes, and release of glucagon-like peptide-1 (GLP-1) and ghrelin in the digestive system. In fact, substances such as dextromethorphan, chloroquine, methimazole and probably glimepiride, being agonists of TAS2Rs, lead to these effects. TAS2Rs and taste 1 receptors (TAS1R2/3) are G protein-coupled receptors (GPCR). TAS1R2/3 are responsible for sweet taste perception and may induce GLP-1 release and insulin secretion. Umami taste receptors, belonging to the same superfamily of receptors, perform a similar function with regard to insulin. The sour and salty taste receptors work in a similar way, both being channel receptors sensitive to amiloride. Finally, gene-protein coupled receptor 40 (GPR40) and GPR120 for fatty taste perception are also protein-coupled receptors and may induce GLP-1 secretion and insulin release, similar to those of other receptors belonging to the same superfamily.

Application In Synthesis of 60-56-0, Methimazole is an antithyroid compound found to have antioxidant properties. Methimazole inhibits activation of the IFN-g-induced Janus kinase (JAK)/STAT signaling pathway in FRTL-5 thyroid cells, which may account for its immunodolulatory effects. Additionally, methimazole is an inhibitor of thyroperoxidase.

Methimazole is a thiourea antithyroid agent that prevents iodine organification, thus inhibiting the synthesis of thyroxine. Antihyperthyroid.

Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%.3 It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat. Methimazole has been used to induce hypothyroidism in mice. Formulations containing methimazole have been used in the treatment of hyperthyroidism.

Methimazole is a thyreostatic compound, and an antihormone, which is widely used in medicine for the treatment of hyperthyroidism.

Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO), with antithyroid activity. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).

Methimazole is an antithyroid medication which is now considered the first line agent for medical therapy of hyperthyroidism and Graves disease. Methimazole has been linked to serum aminotransferase elevations during therapy as well as to a clinically apparent, idiosyncratic liver injury that is typically cholestatic and self-limited in course.
Methimazole, also known as tapazole or danantizol, belongs to the class of organic compounds known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group. Methimazole is a drug which is used for the treatment of hyperthyroidism, goiter, graves disease and psoriasis. Methimazole is soluble (in water) and a very weakly acidic compound (based on its pKa). Methimazole has been detected in multiple biofluids, such as urine and blood. Methimazole can be converted into methimazole S-oxide., 60-56-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents. Category: imidazoles-derivatives.

Dudina, M A;Dogadin, S A;Savchenko, A A;Belenyuk, V D research published 《 [T-lymphocytes phenotypic composition of peripheral blood in patients with Graves’ disease undergoing conservative therapy with thiamazole].》, the research content is summarized as follows. BACKGROUND: Effective control of autoimmune inflammation in Graves’ disease determines necessity to study the T helper (Th) and cytotoxic T-lymphocytes dysfunction, as well as the level of regulatory T-cells (Treg) activation in patients with Graves’ disease on thyrostatic medication, which will clarify the immunomodulatory effects of long-term thiamazole treatment serve as targets for more specific therapies. AIM: To study the phenotypic composition of T-lymphocytes in the peripheral blood of patients with Graves’ disease to assess the direction of immune response depending on thimazole-induced euthyroidism duration. MATERIALS AND METHODS: A single-center, cohort, continuous, open-label, controlled trial was conducted to assess the phenotypic composition of T-lymphocytes in peripheral blood in women with Graves’ disease on long-term thiamazole treatment. The phenotypic composition of T-lymphocytes was determined by flow cytometry using direct immunofluorescence with conjugated FITC monoclonal antibodies depending on the duration of thimazole-induced euthyroidism of long-term thiamazole treatment. RESULTS: The study included 135 women with Graves’ disease, mean age 43.09±12.81 years, 120 (88.91%) with a relapse of the disease and 15 (11.09%) with newly diagnosed hyperthyroidism. An increase of activated CD3+CD4+CD25+ was found in patients with Graves’ disease with a duration of thimazole-induced euthyroidism 5-8 months and 9-12 months, respectively, Me=0.94 (0.48-1.45), p=0.020) and Me=0.95 (0.41-1.80), p=0.025), in control group – Me=0.12 (0.03-0.68). Compared to the control an increase of CD4+CD25+CD127Low (Treg) was found in patients with a duration of thimazole-induced euthyroidism 5-8 and 9-12 months. The content of Treg in peripheral blood in Graves’ disease patients with a duration of thimazole-induced euthyroidism more than 12 months decreases, but remains elevated relative to the control. CONCLUSION: In patients with Graves’ disease with a duration of thimazole-induced euthyroidism 5-8 months and 9-12 months the level of Treg has been increased. The increase of activated Th (CD3+CD4+CD25+) persists independently of thimazole-induced euthyroidism. In patients with Graves’ disease with a duration of thimazole-induced euthyroidism for more than 12 months, there is a compensatory increase in regulatory T-lymphocyte, and the total number of T-helpers is restored to the control.

60-56-0, Methimazole is an antithyroid compound found to have antioxidant properties. Methimazole inhibits activation of the IFN-g-induced Janus kinase (JAK)/STAT signaling pathway in FRTL-5 thyroid cells, which may account for its immunodolulatory effects. Additionally, methimazole is an inhibitor of thyroperoxidase.

Methimazole is a thiourea antithyroid agent that prevents iodine organification, thus inhibiting the synthesis of thyroxine. Antihyperthyroid.

Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%.3 It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat. Methimazole has been used to induce hypothyroidism in mice. Formulations containing methimazole have been used in the treatment of hyperthyroidism.

Methimazole is a thyreostatic compound, and an antihormone, which is widely used in medicine for the treatment of hyperthyroidism.

Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO), with antithyroid activity. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).

Methimazole is an antithyroid medication which is now considered the first line agent for medical therapy of hyperthyroidism and Graves disease. Methimazole has been linked to serum aminotransferase elevations during therapy as well as to a clinically apparent, idiosyncratic liver injury that is typically cholestatic and self-limited in course.
Methimazole, also known as tapazole or danantizol, belongs to the class of organic compounds known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group. Methimazole is a drug which is used for the treatment of hyperthyroidism, goiter, graves disease and psoriasis. Methimazole is soluble (in water) and a very weakly acidic compound (based on its pKa). Methimazole has been detected in multiple biofluids, such as urine and blood. Methimazole can be converted into methimazole S-oxide., Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole based anticancer drug find applications in cancer chemotherapy. 10111-08-7, formula is C4H4N2O, Name is 1H-Imidazole-2-carbaldehyde. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC). Category: imidazoles-derivatives.

Du, Xiaoyu;Li, Mengwen;Du, Man;Shen, Ao;Hao, Xiaohui;Yuan, Jiaxin;Ma, Shufeng;Zhao, Yongwei;Hou, Lala;Li, Ziqi;Yang, Yunxu research published 《 A one-pot strategic construction of functionalized nanomaterial ZIF-90-Rhn for stepwise detection and capturing of Ag⁺ and formaldehyde from an aqueous solution》, the research content is summarized as follows. In this work, a new functionalized nanomaterial, ZIF-90-Rhn, was designed, synthesized and characterized. The synthesis was performed by one-pot strategic construction, post-modification and pre-modification synthesis methods. After encapsulating cyanine dye, Cy-N, into ZIF-90-Rhn, a multi-functional complex of ZIF-90-Rhn@Cy-N was successfully obtained and could be used to detect Ag⁺ in dual-signals (fluorescence signal and visual color signal) by forming an intermedial product of ZIF-90-Rhn@Ag⁺/Cy-N in an aqueous solution Subsequently, the intermediate product ZIF-90-Rhn@Ag⁺/Cy-N could detect formaldehyde (FA) via a stepwise redox recognition reaction through dual-signals. A smartphone portable online detection platform for Ag⁺ and FA using Bluetooth for the color changes under visible light was not realized, and the results are consistent with the fluorescence sensing assay results. Moreover, a chitosan non-woven fabric coated with ZIF-90-Rhn@Cy-N on its surface was considered to evaluate its efficient capturing and removing effects on Ag⁺ and FA in a stepwise actual procedure in water.

Category: imidazoles-derivatives, 1H-Imidazole-2-carbaldehyde, also known as 1H-Imidazole-2-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
1H-Imidazole-2-carboxaldehyde is a novel PTP1b inhibitor with potential application to treat type 2 diabetes.
1H-Imidazole-2-carboxaldehyde is a broad-spectrum antimicrobial that has been shown to inhibit the growth of bacteria by interfering with protein synthesis. It binds to the cytosolic protein and receptor molecule, which are involved in the activation of bacterial enzymes. Imidazole-2-carboxaldehyde reacts with anhydrous sodium and copper complex to produce hydrogen bonds, which prevent the formation of the nitrogen atoms necessary for cellular processes. This chemical also has biological properties such as glyoxal, which inhibits bacterial growth by reacting with amino groups on proteins., 10111-08-7.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . 10111-08-7, formula is C4H4N2O, Name is 1H-Imidazole-2-carbaldehyde. In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with an increase of the alkyl chain length of the alcohols. Product Details of C4H4N2O.

Dong, Ji;Huang, Shi-sheng;Hao, Ya-nan;Wang, Zi-wen;Liu, Yu-xiu;Li, Yong-qiang;Wang, Qing-min research published 《 Marine-natural-products for biocides development: first discovery of meridianin alkaloids as antiviral and anti-phytopathogenic-fungus agents》, the research content is summarized as follows. BACKGROUND : Food is an important strategic material related to national economy and people’s livelihood. In this work, meridianin alkaloids were selected as the parent structure. A series of meridianin alkaloid analogs were rationally designed, synthesized and evaluated for their antiviral activities and fungicidal activities. RESULT : These compounds were found to have good antiviral and fungicidal activities for the first time. The structure-activity relationship (SAR) research revealed that introducing bromine atom at the 5-position of indole ring is beneficial to antiviral activity, but introducing methoxy group is not conducive. Introducing bromine atom at the 6-position of indole ring or nitrogen atom at the 7-position of the indole ring resulted in lower antiviral activity. Most of the meridianin derivatives showed higher anti-TMV activities at 500μg mL^-1 than Ribavirin, especially for compounds 6c, 8a and 10a. All of the compounds also displayed broad spectrum fungicidal activities against 14 kinds of phytopathogenic fungi at 50μg mL^-1. CONCLUSION : Compound 6c with relatively simple structure and excellent antiviral activity, which is similar to that of Ningnanmycin, emerged as novel anti-TMV lead compound Compound 5d with broad spectrum and high effect fungicidal activity emerged as a new fungicidal lead compound Current research lays a solid foundation for the application of meridianin alkaloids in crop protection.

Product Details of C4H4N2O, 1H-Imidazole-2-carbaldehyde, also known as 1H-Imidazole-2-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
1H-Imidazole-2-carboxaldehyde is a novel PTP1b inhibitor with potential application to treat type 2 diabetes.
1H-Imidazole-2-carboxaldehyde is a broad-spectrum antimicrobial that has been shown to inhibit the growth of bacteria by interfering with protein synthesis. It binds to the cytosolic protein and receptor molecule, which are involved in the activation of bacterial enzymes. Imidazole-2-carboxaldehyde reacts with anhydrous sodium and copper complex to produce hydrogen bonds, which prevent the formation of the nitrogen atoms necessary for cellular processes. This chemical also has biological properties such as glyoxal, which inhibits bacterial growth by reacting with amino groups on proteins., 10111-08-7.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole based anticancer drug find applications in cancer chemotherapy. 1739-84-0, formula is C5H8N2, Name is 1,2-Dimethyl-1H-imidazole. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC). Recommanded Product: 1,2-Dimethyl-1H-imidazole.

Domanski, Michal;Zurauskas, Jonas;Barham, Joshua P. research published 《 Tunable Microwave Flow System for Scalable Synthesis of Alkyl Imidazolium-type Ionic Liquids》, the research content is summarized as follows. A continuous flow auto-frequency tuning single-mode microwave reactor is disclosed as a powerful platform to synthesize alkyl imidazolium salts, e.g., I and II, as ionic liquids/ionic liquid precursors in up to near-quant. yields, 100-600 g h^-1 productivities with record space-time yields. Challenges faced, including viscosity changes, dielec. property changes, and phase separation, were addressed by different operation modes of the reactor without reactor redesigning. Depending on the purpose, this highly productive method could prove to be useful for intensive applications of ionic liquids

1739-84-0, 1,2-Dimethylimidazole is used in the synthesis of 1,2-dimethyl-3-n-butylimidazoliumchloride and 1,2-dimethyl-3-n-propylimidazolium chloride. It also can be used in the synthesis of 1-(2-methoxyethyl)-2,3-dimethylimidazolium chloride and hexafluorophosphate salts.
1,2-Dimethylimidazole is a heterocyclic compound that contains nitrogen and carbon. It can be produced by the reaction between glyoxal and fatty acid in the presence of a base. 1,2-Dimethylimidazole has been shown to have biological properties such as an antioxidant effect. It is also used as a chemical intermediate for production of other chemicals such as 2-methylimidazole and 3-methylimidazole. 1,2-Dimethylimidazole has been shown to react with metal carbonyls to produce methylimines, which are useful intermediates in organic synthesis. The reaction mechanism involves hydrogen bonding and steric interactions between the imidazole ring and the metal carbonyl reactant., Recommanded Product: 1,2-Dimethyl-1H-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole based anticancer drug find applications in cancer chemotherapy. 3034-50-2, formula is C4H4N2O, Name is Imidazole-4-carbaldehyde. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC). HPLC of Formula: 3034-50-2.

Ding, Zhongpeng;Li, Feifei;Zhong, Changjiang;Li, Feng;Liu, Yuqian;Wang, Shixiao;Zhao, Jianchun;Li, Wenbao research published 《 Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer》, the research content is summarized as follows. To developed more potent anti-microtubule and cytotoxic derivatives, the co-crystal complexes of plinabulin derivatives (I) [R = H, Me, cyclopropyl, iso-Pr, tert-butyl; X = O, CO] and (II) [R¹= 2-furyl, cyclohexyl, 2-benzoimidazolyl, etc.; X = O; R¹= 5-methyl-2-furyl, 5-methoxymethyl-2-furyl; X = CO] were summarized and analyzed. The further modifications were performed the tert-Bu moiety or C-ring of imidazole-type derivatives to build a library of mols. through the introduction of different groups for novel skeletons. Our structure-activity relationship study indicated that compounds (II) [R¹= 5-methoxymethyl-2-furyl, X = O] (IC₅₀= 14.0 nM, NCI-H460) and [R¹= 5-methoxymethyl-2-furyl, X = CO] (IC₅₀= 2.9 nM, NCI-H460) with furan groups exhibited potent cytotoxic activities at the nanomolar level against various human cancer cell lines. In particular, the 5-Me or methoxymethyl substituent of furan group could replace the alkyl group of imidazole at the 5-position to maintain cytotoxic activity, contradicting previous reports that the tert-Bu moiety at the 5-position of imidazole was essential for the activity of such compounds Immunofluorescence assay indicated that compounds II [R¹= 5-methoxymethyl-2-furyl, X = O, CO] could efficiently inhibited microtubule polymerization Overall, the novel furan-diketopiperazine-type derivatives I and II could be considered as a potential scaffold for the development of anti-cancer drugs.

3034-50-2, 1H-Imidazole-4-carbaldehyde, also known as 1H-Imidazole-4-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
The starting material for a practical synthesis of a potent C17,20-lyase inhibitor. The lyase is a key enzyme in androgen biosynthesis as well as a target for treatment of androgen-dependent prostate cancer. Used to synthesize potent antimalarial drug.
1H-Imidazole-4-carbaldehyde is a chemical compound that has been shown to bind to the glucocorticoid receptor. It was synthesized by reacting 1,2-diaminobenzene with formaldehyde and then hydrolyzing the intermediate imidazolium salt, which is stable in acidic solutions. The complex can be prepared by mixing two solutions of imidazole and trifluoroacetic acid. The ligand has a redox potential of -0.1 V (vs NHE). This means it can be oxidized to the carbonyl group or reduced back to the imidazole ring. The compound is stable in neutral solution and forms stable complexes with metal ions such as Cu+, Fe3+, and Zn2+. It also coordinates well with oxygen atoms, nitrogen atoms, and water molecules. 1H-Imidazole-4-carbaldehyde has been shown to bind to glucocortic, HPLC of Formula: 3034-50-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole based anticancer drug find applications in cancer chemotherapy. 10111-08-7, formula is C4H4N2O, Name is 1H-Imidazole-2-carbaldehyde. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC). Name: 1H-Imidazole-2-carbaldehyde.

Ding, Zhongpeng;Li, Feifei;Zhong, Changjiang;Li, Feng;Liu, Yuqian;Wang, Shixiao;Zhao, Jianchun;Li, Wenbao research published 《 Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer》, the research content is summarized as follows. To developed more potent anti-microtubule and cytotoxic derivatives, the co-crystal complexes of plinabulin derivatives (I) [R = H, Me, cyclopropyl, iso-Pr, tert-butyl; X = O, CO] and (II) [R¹= 2-furyl, cyclohexyl, 2-benzoimidazolyl, etc.; X = O; R¹= 5-methyl-2-furyl, 5-methoxymethyl-2-furyl; X = CO] were summarized and analyzed. The further modifications were performed the tert-Bu moiety or C-ring of imidazole-type derivatives to build a library of mols. through the introduction of different groups for novel skeletons. Our structure-activity relationship study indicated that compounds (II) [R¹= 5-methoxymethyl-2-furyl, X = O] (IC₅₀= 14.0 nM, NCI-H460) and [R¹= 5-methoxymethyl-2-furyl, X = CO] (IC₅₀= 2.9 nM, NCI-H460) with furan groups exhibited potent cytotoxic activities at the nanomolar level against various human cancer cell lines. In particular, the 5-Me or methoxymethyl substituent of furan group could replace the alkyl group of imidazole at the 5-position to maintain cytotoxic activity, contradicting previous reports that the tert-Bu moiety at the 5-position of imidazole was essential for the activity of such compounds Immunofluorescence assay indicated that compounds II [R¹= 5-methoxymethyl-2-furyl, X = O, CO] could efficiently inhibited microtubule polymerization Overall, the novel furan-diketopiperazine-type derivatives I and II could be considered as a potential scaffold for the development of anti-cancer drugs.

Name: 1H-Imidazole-2-carbaldehyde, 1H-Imidazole-2-carbaldehyde, also known as 1H-Imidazole-2-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
1H-Imidazole-2-carboxaldehyde is a novel PTP1b inhibitor with potential application to treat type 2 diabetes.
1H-Imidazole-2-carboxaldehyde is a broad-spectrum antimicrobial that has been shown to inhibit the growth of bacteria by interfering with protein synthesis. It binds to the cytosolic protein and receptor molecule, which are involved in the activation of bacterial enzymes. Imidazole-2-carboxaldehyde reacts with anhydrous sodium and copper complex to produce hydrogen bonds, which prevent the formation of the nitrogen atoms necessary for cellular processes. This chemical also has biological properties such as glyoxal, which inhibits bacterial growth by reacting with amino groups on proteins., 10111-08-7.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. 3034-50-2, formula is C4H4N2O, Name is Imidazole-4-carbaldehyde. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents. Computed Properties of 3034-50-2.

Ding, Chong-Wei;Luo, Wenzhi;Zhou, Jie-Yi;Ma, Xin-Jie;Chen, Guang-Hui;Zhou, Xiao-Ping;Li, Dan research published 《 Hydroxo Iron(III) Sites in a Metal-Organic Framework: Proton-Coupled Electron Transfer and Catalytic Oxidation of Alcohol with Molecular Oxygen》, the research content is summarized as follows. Metalloenzymes are powerful biocatalysts that can catalyze particular chem. reactions with high activity, selectivity, and specificity under mild conditions. Metal-organic frameworks (MOFs) composed of metal ions or metal clusters and organic ligands with defined cavities have the potential to impart enzyme-like catalytic activity and mimic metalloenzymes. Here, a new metal-organic framework implanted with hydroxo iron(III) sites with the structural and reactivity characteristics of iron-containing lipoxygenases is reported. Similar to lipoxygenases, the hydrogen atoms and electrons of the substrate can transfer to the hydroxo iron(III) sites, showing typical proton-coupled electron transfer behavior. In the reactivity mimicking biol. system, similar to alc. oxidase, the material also catalyzes the oxidation of alc. into aldehyde by using O₂ with a high yield and 100% selectivity under mild conditions, without the use of a radical cocatalyst or photoexcitation. These results provide strong evidence for the high structural fidelity of enzymically active sites in MOF materials, verifying that MOFs provide an ideal platform for designing biomimetic heterogeneous catalysts with high conversion efficiency and product selectivity.

Computed Properties of 3034-50-2, 1H-Imidazole-4-carbaldehyde, also known as 1H-Imidazole-4-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
The starting material for a practical synthesis of a potent C17,20-lyase inhibitor. The lyase is a key enzyme in androgen biosynthesis as well as a target for treatment of androgen-dependent prostate cancer. Used to synthesize potent antimalarial drug.
1H-Imidazole-4-carbaldehyde is a chemical compound that has been shown to bind to the glucocorticoid receptor. It was synthesized by reacting 1,2-diaminobenzene with formaldehyde and then hydrolyzing the intermediate imidazolium salt, which is stable in acidic solutions. The complex can be prepared by mixing two solutions of imidazole and trifluoroacetic acid. The ligand has a redox potential of -0.1 V (vs NHE). This means it can be oxidized to the carbonyl group or reduced back to the imidazole ring. The compound is stable in neutral solution and forms stable complexes with metal ions such as Cu+, Fe3+, and Zn2+. It also coordinates well with oxygen atoms, nitrogen atoms, and water molecules. 1H-Imidazole-4-carbaldehyde has been shown to bind to glucocortic, 3034-50-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. Their solubility in alcohol is lower than that in water and decreases with increasing molecular weight of the alcohols . Safety of 1-Methyl-1H-imidazole-2(3H)-thione.

di Filippo, Luigi;Castellino, Laura;Giustina, Andrea research published 《 Occurrence and response to treatment of Graves’ disease after COVID vaccination in two male patients》, the research content is summarized as follows. COVID-19 had dramatic impact worldwide and various vaccines anti-SARS-CoV-2 were rapidly developed. Despite a good safety profile in clin. trials, rare and severe side effects of vaccines have been reported, including thyroid dysfunctions. In particular, occurrence of Graves’ disease (GD) post-vaccination with Tozinameran (Pfizer-BioNTech) was reported in three female subjects and only one male prevalently in young-adult age somewhat reflecting the epidemiol. age and sex distribution of the disease. Reported here is the occurrence and the response to treatment of GD in two male patients after Vaxzevria (Oxford-AstraZeneca) SARS-CoV-2 vaccinations. Case 1 is of a previously healthy, past-smoker, 32-yr-old male patient, without any personal or family history of endocrine and autoimmune diseases, ten days after the second dose of Vaxzevria vaccine developed anxiety, tachycardia and palpitations, without signs of orbitopathy or local pain. Tyroid-function tests revealed decreased TSH with elevated free-T4 and free-T3 levels and elevated thy rotropin recept or-antibodies (TRAbs). After three months of therapy his thyroid function is currently normal and TRAbs levels halved on 100 mg/daily dose of propylthiouracil. Case 2 is of a reviously healthy, past-smoker, 35-yr-old male patient, without any personal or family history of endocrine and autoimmune disease, 5 days after the first dose of Vaxzevria vaccine developed headache, nausea, asthenia, palpitations, tachycardia, mild eyes-redness and superior palpebral retraction. Thyroid-function tests revealed sup- pressed TSH with elevated free-T4 and free-T3 levels and elevated TRAbs. After three months of therapy his thyroid function and TRAbs levels are currently normal on 5 mg/daily dose of thiamazole. It cannot be excluded also a possible influence of vitamin D status on GD occurrence after COVID-19 vaccination, although data on VD status in our patients were not available. In conclusion, although COVID-19 vaccination is currently not contraindicated in patients with stable autoimmune endocrine diseases,this data suggest a note of caution in administering a further vaccine dose to patients that developed GD in the first weeks after vaccination. Moreover, it is suggested to carefully consider if submitting patients with recent onset or non-stable GD to all types of COVID-19 vaccination.

60-56-0, Methimazole is an antithyroid compound found to have antioxidant properties. Methimazole inhibits activation of the IFN-g-induced Janus kinase (JAK)/STAT signaling pathway in FRTL-5 thyroid cells, which may account for its immunodolulatory effects. Additionally, methimazole is an inhibitor of thyroperoxidase.

Methimazole is a thiourea antithyroid agent that prevents iodine organification, thus inhibiting the synthesis of thyroxine. Antihyperthyroid.

Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%.3 It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat. Methimazole has been used to induce hypothyroidism in mice. Formulations containing methimazole have been used in the treatment of hyperthyroidism.

Methimazole is a thyreostatic compound, and an antihormone, which is widely used in medicine for the treatment of hyperthyroidism.

Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO), with antithyroid activity. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).

Methimazole is an antithyroid medication which is now considered the first line agent for medical therapy of hyperthyroidism and Graves disease. Methimazole has been linked to serum aminotransferase elevations during therapy as well as to a clinically apparent, idiosyncratic liver injury that is typically cholestatic and self-limited in course.
Methimazole, also known as tapazole or danantizol, belongs to the class of organic compounds known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group. Methimazole is a drug which is used for the treatment of hyperthyroidism, goiter, graves disease and psoriasis. Methimazole is soluble (in water) and a very weakly acidic compound (based on its pKa). Methimazole has been detected in multiple biofluids, such as urine and blood. Methimazole can be converted into methimazole S-oxide., Safety of 1-Methyl-1H-imidazole-2(3H)-thione

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Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem