Tag: 100-200

《TAT-functionalized PEI-grafting rice bran polysaccharides for safe and efficient gene delivery》 was written by Liu, Liang; Yan, Yujian; Ni, Danni; Wu, Shuheng; Chen, Yiran; Chen, Xin; Xiong, Xuemin; Liu, Gang. Safety of Di(1H-imidazol-1-yl)methanone And the article was included in International Journal of Biological Macromolecules in 2020. The article conveys some information:

Polysaccharides are considered to be promising candidates for non-viral gene delivery because of their mol. diversity, which can be modified to fine-tune their physicochem. properties. In this work, transcriptional activator protein (TAT) functionalized PEI grafted polysaccharide polymer (PRBP) was prepared by using rice bran polysaccharide as the starting material, and characterized by various methods. The potential of TAT functionalized PRBP (PRBP-TAT) as gene vector was studied in vitro, including DNA loading capacity, DNA protection ability and biocompatibility. The cell uptake and transfection efficiency of the PRBP-TAT/pDNA polyplexes were studied. The results showed that PRBP-TAT could completely condense DNA at N/P 2. The PRBP-TAT/pDNA polyplexes could protect DNA from degrading by DNase and were efficiently internalized by cells. Biocompatibility result showed that PRBP-TAT had no significant cytotoxicity and effect on cell proliferation. At low N/P ratios of 1-3.5, PRBP-TAT showed higher transfection efficiency than PEI30k and PEI30k-grafted rice bran polysaccharide. PRBP-TAT and PEI showed the highest transfection efficiency of 42.8% and 28.1% when pDNA is 2 ug and N/P ratio is 1.5, resp., while PRBP showed the highest transfection efficiency of 37.3% at N/P 2.5. These results indicate that PTA is a promising candidate vector for safe and efficient gene delivery. In the experiment, the researchers used many compounds, for example, Di(1H-imidazol-1-yl)methanone(cas: 530-62-1Safety of Di(1H-imidazol-1-yl)methanone)

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a peptide coupling reagent,it is used in the synthesis of peptides. Reacts readily with carboxylic acids to form acyl imidazoles; subsequent reaction with amines to form amides goes smoothly.Safety of Di(1H-imidazol-1-yl)methanone

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《Hyperbranched cationic polysaccharide derivatives for efficient siRNA delivery and diabetic wound healing enhancement》 was published in International Journal of Biological Macromolecules in 2020. These research results belong to Lan, Biyun; Wu, Junfeng; Li, Na; Pan, Chenglin; Yan, Li; Yang, Chuan; Zhang, Liming; Yang, Liqun; Ren, Meng. Computed Properties of C7H6N4O The article mentions the following:

Gene vectors are important for successful siRNA delivery. Four types of hyperbranched cationic polysaccharide derivatives (HCP) were synthesized by conjuncting 1,2-ethylenediamine (EDA) and diethylenetriamine (DETA) with glycogen or amylopectin resp. and named as G-EDA, G-DETA, A-EDA and A-DETA. The efficiency and safety of these HCPs to deliver siRNA were explored in vitro and in vivo. Our results showed that HCPs could form complexes with siRNA. All HCP/siRNA exhibited negligible cytotoxicity. Compared with A-EDA and A-DETA, G-EDA and G-DETA could carry much more siRNA into cells and then escape from endosomes. The delivery of MMP-9 siRNA (siMMP-9) by G-EDA and G-DETA significantly inhibited MMP-9 in HaCaT cells. Wound models in diabetic rats demonstrated that treatment of G-EDA/siMMP-9 could potently knock down MMP-9 of skin wound tissues and then enhanced wound healing. In summary, this study provided an effective and safe approach for siRNA delivery in vitro and in vivo.Di(1H-imidazol-1-yl)methanone(cas: 530-62-1Computed Properties of C7H6N4O) was used in this study.

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a peptide coupling reagent,it is used in the synthesis of peptides. Reacts readily with carboxylic acids to form acyl imidazoles; subsequent reaction with amines to form amides goes smoothly.Computed Properties of C7H6N4O

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The author of 《Nanostructured γ-Fe2O3@Starch-n-Butyl SO3H as new recyclable magnetic catalyst for promoting multi-component reactions》 were Shamsi-Sani, Mahnaz; Shirini, Farhad; Mohammadi-Zeydi, Masoud. And the article was published in Journal of Nanoscience and Nanotechnology in 2019. Application In Synthesis of 1H-Benzo[d]imidazol-2-amine The author mentioned the following in the article:

Butane-1-soltunic acid modified starch-coated γ-Fe2O3 magnetic nanoparticles [γ-Fe2O3@starch- Bu SO3H] was easily prepared through a ring opening reaction of 1,4-butane sultone with nano- magnetic γ-Fe2O3@starch. After structural studies, using FT-IR, SEM, XRD, TGA, TEM, EDX, VSM and also pH anal. the efficiency of this reagent in the preparation of tetrahydrobenzinnidazo[2,1-b] quinazolin-1(2H)-ones and 2H-indazolo[2,1-b]phthalazine-triones was studied. Operational simple- ness, high yields, short reaction times, wide applicability and simple recyclability of the catalyst employing an external magnet are the most important advantages of this methodol. The experimental part of the paper was very detailed, including the reaction process of 1H-Benzo[d]imidazol-2-amine(cas: 934-32-7Application In Synthesis of 1H-Benzo[d]imidazol-2-amine)

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.Application In Synthesis of 1H-Benzo[d]imidazol-2-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2011,Abul Hashem, Md.; Sultana, Abeda published 《Synthesis of N-(2′-imidazolyl)-2-aminopyridyl palladium dichloride and its application as catalyst in Suzuki-Miyaura cross coupling reaction》.Journal of the Bangladesh Chemical Society published the findings.Synthetic Route of C3H3BrN2 The information in the text is summarized as follows:

The ligand N-(2′-imidazolyl)-2-aminopyridine was prepared from imidazole and it forms N-(2′-imidazolyl)-2-aminopyridyl palladium dichloride complex with Na2PdCl4 in methanol. The complex (1.5 mmol %) was used to prepare substituted biphenyls, terphenyls, and heterobiaryls in good to excellent yields via Suzuki-Miyaura cross-coupling reaction of substituted phenylboronic acids and substituted aryl chlorides, bromides and iodides. The experimental part of the paper was very detailed, including the reaction process of 2-Bromo-1H-imidazole(cas: 16681-56-4Synthetic Route of C3H3BrN2)

2-Bromo-1H-imidazole(cas: 16681-56-4) is a member of imidazole. Its exclusive structural characteristics with enviable electron-rich features are favorable for imidazole-based fused heterocycles to bind efficiently with an array of enzymes and receptors in biological systems through various weak interactions like hydrogen bonds, ion-dipole, cation-π, π-π stacking, coordination, Van der Waals forces, hydrophobic effects, etc., and therefore they demonstrate widespread bioactivities. Synthetic Route of C3H3BrN2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2008,Angell, Richard M.; Angell, Tony D.; Bamborough, Paul; Brown, David; Brown, Murray; Buckton, Jacky B.; Cockerill, Stuart G.; Edwards, Chris D.; Jones, Katherine L.; Longstaff, Tim; Smee, Penny A.; Smith, Kathryn J.; Somers, Don O.; Walker, Ann L.; Willson, Malcolm published 《Biphenyl amide p38 kinase inhibitors. 2: Optimization and SAR》.Bioorganic & Medicinal Chemistry Letters published the findings.Recommanded Product: 16681-56-4 The information in the text is summarized as follows:

The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38α are discussed with reference to the x-ray crystal structure of an example. The series was optimized rapidly to a compound (I) showing oral activity in an in vivo disease model. After reading the article, we found that the author used 2-Bromo-1H-imidazole(cas: 16681-56-4Recommanded Product: 16681-56-4)

2-Bromo-1H-imidazole(cas: 16681-56-4) is a member of imidazole. Its exclusive structural characteristics with enviable electron-rich features are favorable for imidazole-based fused heterocycles to bind efficiently with an array of enzymes and receptors in biological systems through various weak interactions like hydrogen bonds, ion-dipole, cation-π, π-π stacking, coordination, Van der Waals forces, hydrophobic effects, etc., and therefore they demonstrate widespread bioactivities. Recommanded Product: 16681-56-4

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《2-aminobenzimidazoles for leishmaniasis: From initial hit discovery to in vivo profiling》 was written by Ferreira, Rafael Augusto Alves; Junior, Celso de Oliveira Rezende; Martinez, Pablo David Grigol; Koovits, Paul John; Soares, Bruna Miranda; Ferreira, Leonardo L. G.; Michelan-Duarte, Simone; Chelucci, Rafael Consolin; Andricopulo, Adriano D.; Galuppo, Mariana K.; Uliana, Silvia R. B.; Matheeussen, An; Caljon, Guy; Maes, Louis; Campbell, Simon; Kratz, Jadel M.; Mowbray, Charles E.; Dias, Luiz Carlos. Recommanded Product: 1H-Benzo[d]imidazol-2-amine And the article was included in PLoS Neglected Tropical Diseases in 2021. The article conveys some information:

Leishmaniasis is a major infectious disease with hundreds of thousands of new cases and over 20,000 deaths each year. The current drugs to treat this life-threatening infection have several drawbacks such as toxicity and long treatment regimens. A library of 1.8 million compounds, from which the hits reported here are publicly available, was screened against Leishmania infantum as part of an optimization program; a compound was found with a 2-aminobenzimidazole functionality presenting moderate potency, low metabolic stability and high lipophilicity. Several rounds of synthesis were performed to incorporate chem. groups capable of reducing lipophilicity and clearance, leading to the identification of compounds that are active against different parasite strains and have improved in vitro properties. As a result of this optimization program, a group of compounds was further tested in anticipation of in vivo evaluation. In vivo tests were carried out with compounds 29 (L. infantum IC50: 4.1 μM) and 39 (L. infantum IC50: 0.5 μM) in an acute L. infantum VL mouse model, which showed problems of poor exposure and lack of efficacy, despite the good in vitro potency. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d]imidazol-2-amine(cas: 934-32-7Recommanded Product: 1H-Benzo[d]imidazol-2-amine)

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.Recommanded Product: 1H-Benzo[d]imidazol-2-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The author of 《Hydrogen bonding promoted simple and clean photo-induced reduction of C-X bond with isopropanol》 were Cao, Dawei; Yan, Chaoxian; Zhou, Panpan; Zeng, Huiying; Li, Chao-Jun. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2019. Name: 2-Chloro-1H-benzo[d]imidazole The author mentioned the following in the article:

We herein report a simple and clean photo-induced metal-free reduction of C-X bond under an atm. of air at room temperature Isopropanol is used as both the reducing reagent and solvent [e.g., Me 4-iodobenzoate → Me benzoate (96%) under UV irradiation in isopropanol]. Various functional groups (acids, esters, alcs., anilines, phenols, indoles, pyridines, cyano and trifluoromethyl groups) and other heterocyclic compounds are tolerated. Different organic halides (including C-I, C-Br and C-Cl bonds) can be dehalogenated with moderate to excellent yields. Polyhalides are also reduced chemoselectively and efficiently. DFT calculation suggests a six-membered ring transition state via C-X···H-O hydrogen bonding to decrease the activation energy. After reading the article, we found that the author used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Name: 2-Chloro-1H-benzo[d]imidazole)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) is an analog of benzimidazole that has been synthesized by Langmuir adsorption isotherm. It is a white crystalline solid that can be dissolved in water and hydrochloric acid. 2-Chloro-1H-benzo[d]imidazole inhibits the growth of herpes simplex virus by acting as a competitive inhibitor for the viral enzyme thymidine kinase, which catalyzes the conversion of thymine to thymidine.Name: 2-Chloro-1H-benzo[d]imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The author of 《Aggregation-induced emission: lighting up herg potassium channel》 were Zhang, Xiaomeng; Liu, Tingting; Li, Qi; Li, Minyong; Du, Lupei. And the article was published in Frontiers in Chemistry (Lausanne, Switzerland) in 2019. Category: imidazoles-derivatives The author mentioned the following in the article:

Based on the scaffold of astemizole and E-4031, four AIE light-up probes (L1-L4) for Human Ether-a-go-go-Related Gene (hERG) potassium channel were developed herein using AIE fluorogen(TPE). These probes showing advantages such as low background interference, superior photostability, acceptable cell toxicity, and potent inhibitory activity, which could be used to image hERG channels at the nanomolar level. These AIE light-up probes hoped to provide guidelines for the design of more advanced AIE sensing and imaging hERG channels to a broad range of applications. In the experiment, the researchers used many compounds, for example, 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Category: imidazoles-derivatives)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) is an analog of benzimidazole that has been synthesized by Langmuir adsorption isotherm. It is a white crystalline solid that can be dissolved in water and hydrochloric acid. 2-Chloro-1H-benzo[d]imidazole inhibits the growth of herpes simplex virus by acting as a competitive inhibitor for the viral enzyme thymidine kinase, which catalyzes the conversion of thymine to thymidine.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2019,Analytical Chemistry (Washington, DC, United States) included an article by Wu, Yafeng; Zhang, Fen; Wang, Kan; Luo, Peicheng; Wei, Yuanqing; Liu, Songqin. Category: imidazoles-derivatives. The article was titled 《Activatable Fluorescence Imaging and Targeted Drug Delivery via Extracellular Vesicle-Like Porous Coordination Polymer Nanoparticles》. The information in the text is summarized as follows:

Cancer imaging with minimal background signal and targeted intracellular drug delivery are of vital importance in clin. cancer diagnosis and therapy. Herein, we developed a biomimetic nanoprobe for activated fluorescence imaging and targeted drug delivery. PH-responsive porous coordination polymer nanoparticles (PCP NPs) were first synthesized by a codeposition method, anticancer drug doxorubicin (DOX) was then loaded into PCP NPs through phys. and electrostatic adsorption (PCP-DOX), and finally the cell membranes extracted from Bel-7402 cancer cells were coated on the DOX-loaded PCP NPs (PCP-DOX-CM). The fluorescence of DOX was quenched due to the fluorescence resonance energy transfer between DOX and PCP NPs. Under acidic environment inside cancer cells, PCP NPs degraded, DOX was released from PCP-DOX-CM, and the fluorescence of DOX was activated, which was very specific for cancers with a high signal-to-noise ratio. Benefited from immune escaping and homologous targeting ability from cancer cell membranes, compared with PCP-CM and PCP-DOX, PCP-DOX-CM significantly enhanced the cellular endocytosis of DOX in Bel-7402 cancer cells and exhibited excellent cancer therapy effect in vitro. Together, our work provides a useful platform for an activated cancer imaging system and personalized cancer treatment. After reading the article, we found that the author used Di(1H-imidazol-1-yl)methanone(cas: 530-62-1Category: imidazoles-derivatives)

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a peptide coupling reagent,it is used in the synthesis of peptides. Reacts readily with carboxylic acids to form acyl imidazoles; subsequent reaction with amines to form amides goes smoothly.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2017,Qian, Ping; Deng, Yu; Mei, Haibo; Han, Jianlin; Pan, Yi published 《Metal-free nitroxyl radical-mediated β-C(sp3)-H amination of saturated ketones with heteroaryl halides: multiple roles of TEMPO》.Chemical Communications (Cambridge, United Kingdom) published the findings.Recommanded Product: 2-Chloro-1H-benzo[d]imidazole The information in the text is summarized as follows:

The first metal-free nitroxyl-radical-mediated β-amination of saturated ketones by using heteroaryl halides as amide precursors has been developed. This reaction proceeds through a cascade α-aminoxylation/Cope-like elimination/aza-Michael addition sequence to afford β-amino ketone derivatives with excellent yields. TEMPO plays multiple roles in the current β-amination process, including those of an oxidant, an α-aminoxylation reagent, a β-hydrogen acceptor, an in situ base, and an oxygen source. In the experiment, the researchers used many compounds, for example, 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Recommanded Product: 2-Chloro-1H-benzo[d]imidazole)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) is an analog of benzimidazole that has been synthesized by Langmuir adsorption isotherm. It is a white crystalline solid that can be dissolved in water and hydrochloric acid. 2-Chloro-1H-benzo[d]imidazole inhibits the growth of herpes simplex virus by acting as a competitive inhibitor for the viral enzyme thymidine kinase, which catalyzes the conversion of thymine to thymidine.Recommanded Product: 2-Chloro-1H-benzo[d]imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem