Category: 4857-06-1

Dziwornu, Godwin Akpeko; Coertzen, Dina; Leshabane, Meta; Korkor, Constance M.; Cloete, Cleavon K.; Njoroge, Mathew; Gibhard, Liezl; Lawrence, Nina; Reader, Janette; van der Watt, Mariette; Wittlin, Sergio; Birkholtz, Lyn-Marie; Chibale, Kelly published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure-Activity Relationship and In Vivo Oral Efficacy Studies》.Formula: C7H5ClN2 The article contains the following contents:

A novel series of antimalarial benzimidazole derivatives incorporating phenolic Mannich base side chains at the C2 position, which possess dual asexual blood and sexual stage activities, is presented. Structure-activity relationship studies revealed that the 1-benzylbenzimidazole analogs possessed submicromolar asexual blood and sexual stage activities in contrast to the 1H-benzimidazole analogs, which were only active against asexual blood stage (ABS) parasites. Further, the former demonstrated microtubule inhibitory activity in ABS parasites but more significantly in stage II/III gametocytes. In addition to being bona fide inhibitors of hemozoin formation, the 1H-benzimidazole analogs also showed inhibitory effects on microtubules. In vivo efficacy studies in Plasmodium berghei-infected mice revealed that the frontrunner compound 41(I) exhibited high efficacy (98% reduction in parasitemia) when dosed orally at 4 × 50 mg/kg. Generally, the compounds were noncytotoxic to mammalian cells. In addition to this study using 2-Chloro-1H-benzo[d]imidazole, there are many other studies that have used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Formula: C7H5ClN2) was used in this study.

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Formula: C7H5ClN2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《Alkylated benzimidazoles: Design, synthesis, docking, DFT analysis, ADMET property, molecular dynamics and activity against HIV and YFV》 was published in Computational Biology and Chemistry in 2020. These research results belong to Srivastava, Ritika; Gupta, Sunil K.; Naaz, Farha; Sen Gupta, Parth Sarthi; Yadav, Madhu; Singh, Vishal Kumar; Singh, Anuradha; Rana, Malay Kumar; Gupta, Satish Kumar; Schols, Dominique; Singh, Ramendra K.. Related Products of 4857-06-1 The article mentions the following:

A series of alkylated benzimidazole derivatives I [R1 = H, Br, NO2; R2 = H, Br, NO2; R3 = (CH2)2OH, (CH2)3OH] was synthesized and screened for their anti-HIV, anti-YFV, and broad-spectrum antiviral properties. The physicochem. parameters and drug-like properties of the compounds were assessed first, and then docking studies and MD simulations on HIV-RT allosteric sites were conducted to find the possible mode of their action. DFT anal. was also performed to confirm the nature of the hydrogen bonding interaction of active compounds The in silico studies indicated that the mols. behaved like possible NNRTIs. The nature – polar or non-polar and position of the substituent present at fifth, sixth, and N-1 positions of the benzimidazole moiety played an important role in determining the antiviral properties of the compounds Among the various compounds, I (R1 = R2 = Br; R3 = (CH2)2OH) showed anti-HIV activity with an appreciably low IC50 value as 0.386 x 10-5μM. Similarly, compound I (R1 = NO2; R2 = H; R3 = (CH2)3OH), showed excellent inhibitory property against the yellow fever virus (YFV) with EC50 value as 0.7824 x 10-2μM. In the experiment, the researchers used many compounds, for example, 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Related Products of 4857-06-1)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Related Products of 4857-06-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Category: imidazoles-derivativesIn 2017 ,《Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Toyota, Yosuke; Nomura, Sayaka; Makishima, Makoto; Hashimoto, Yuichi; Ishikawa, Minoru. The article contains the following contents:

Anti-inflammatory effects of peroxisome proliferator-activated receptor gamma (PPRAγ) ligands are thought to be largely due to PPARγ-mediated transrepression. Thus, transrepression-selective PPARγ ligands without agonistic activity or with only partial agonistic activity should exhibit anti-inflammatory properties with reduced side effects. Here, the authors investigated the structure-activity relationships (SARs) of PPARγ agonist rosiglitazone, focusing on transrepression activity. Alkenic analogs showed slightly more potent transrepression with reduced efficacy of transactivating agonistic activity. Removal of the alkyl group on the nitrogen atom improved selectivity for transrepression over transactivation. Among the synthesized compounds, I exhibited stronger transrepressional activity (IC50: 14 μM) and weaker agonistic efficacy (11%) than rosiglitazone or pioglitazone. After reading the article, we found that the author used 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 2017,D’Attoma, Joseph; Camara, Titi; Brun, Pierre Louis; Robin, Yves; Bostyn, Stephane; Buron, Frederic; Routier, Sylvain published 《Efficient Transposition of the Sandmeyer Reaction from Batch to Continuous Process》.Organic Process Research & Development published the findings.Application In Synthesis of 2-Chloro-1H-benzo[d]imidazole The information in the text is summarized as follows:

The transposition of Sandmeyer chlorination from a batch to a safe continuous flow process was investigated. Our initial approach was to develop a cascade method using flow chem. which involved the generation of diazonium salt and its quenching with copper chloride. To achieve this safe diazotation continuous process, a chemometric approach (Simplex method) was used and extrapolated to establish a fully continuous flow method. The reaction scope was also examined via the synthesis of several (het)aryl chlorines. Validation and scale-up of the process were also performed. A higher productivity was obtained under increasingly tight security. The results came from multiple reactions, including the reaction of 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Application In Synthesis of 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.Application In Synthesis of 2-Chloro-1H-benzo[d]imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2017,Niguez, Diego Ros; Guillena, Gabriela; Alonso, Diego A. published 《Chiral 2-Aminobenzimidazoles in Deep Eutectic Mixtures: Recyclable Organocatalysts for the Enantioselective Michael Addition of 1,3-Dicarbonyl Compounds to β-Nitroalkenes》.ACS Sustainable Chemistry & Engineering published the findings.Related Products of 4857-06-1 The information in the text is summarized as follows:

A catalytic system based on deep eutectic solvents (DESs) and chiral 2-amino benzimidazole organocatalysts is used to promote the enantioselective addition of 1,3-dicarbonyl compounds to β-nitrostyrenes. This procedure avoids the use of toxic volitile organic compounds (VOCs) as a reaction medium, providing access to highly functionalized chiral mols. in a selective and efficient manner. Furthermore, the reaction can be performed on a large scale and recycling the catalytic system is possible for at least four times, leading to a clean, cheap, simple, and scalable procedure that meets most of the criteria required to be a green and sustainable process. NMR studies have confirmed the key role of the hydrogen-bonding interactions between the DES and the chiral organocatalyst, which allow their recovery and the recyclability of the system. In the experiment, the researchers used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Related Products of 4857-06-1)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Related Products of 4857-06-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2017,Niguez, Diego Ros; Guillena, Gabriela; Alonso, Diego A. published 《Chiral 2-Aminobenzimidazoles in Deep Eutectic Mixtures: Recyclable Organocatalysts for the Enantioselective Michael Addition of 1,3-Dicarbonyl Compounds to β-Nitroalkenes》.ACS Sustainable Chemistry & Engineering published the findings.Related Products of 4857-06-1 The information in the text is summarized as follows:

A catalytic system based on deep eutectic solvents (DESs) and chiral 2-amino benzimidazole organocatalysts is used to promote the enantioselective addition of 1,3-dicarbonyl compounds to β-nitrostyrenes. This procedure avoids the use of toxic volitile organic compounds (VOCs) as a reaction medium, providing access to highly functionalized chiral mols. in a selective and efficient manner. Furthermore, the reaction can be performed on a large scale and recycling the catalytic system is possible for at least four times, leading to a clean, cheap, simple, and scalable procedure that meets most of the criteria required to be a green and sustainable process. NMR studies have confirmed the key role of the hydrogen-bonding interactions between the DES and the chiral organocatalyst, which allow their recovery and the recyclability of the system. In the experiment, the researchers used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Related Products of 4857-06-1)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Related Products of 4857-06-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2018,Research on Chemical Intermediates included an article by Srikrishna, Devulapally; Dubey, Pramod Kumar. Electric Literature of C7H5ClN2. The article was titled 《Synthesis of novel substituted 3-(4-((1H-benzo[d]imidazol-2-ylthio)methyl)-1-phenyl-1H-pyrazol-3-yl)-2H-chromen-2-ones: various approaches》. The information in the text is summarized as follows:

Considering benzimidazole as a privileged structure for developing probes of impressive pharmacol. potentials, some new coumarin and pyrazole conjugates of benzimidazoles I (R = Me, Et, Bn; X = H, OMe) were synthesized with a sulfur linkage. Thus, 3-(2-oxo-2H-chromen-3-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde was prepared starting from simple salicylaldehyde which has been used as an important synthon and incorporated in a series of structural manipulations to obtain various pharmacophoric motif conjugates I (R = H, Me, Et, Bn) in fair yields. A facile and stepwise method has been developed for the synthesis of all these compounds in various approaches, which also involves sub-sequences. In addition to this study using 2-Chloro-1H-benzo[d]imidazole, there are many other studies that have used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Electric Literature of C7H5ClN2) was used in this study.

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.Electric Literature of C7H5ClN2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Boehme, Matthias D.; Wilm, Lukas F. B.; Hepp, Alexander; Hahn, F. Ekkehardt published an article in 2021. The article was titled 《Regioselective Double Oxidative Addition of Bis-NHC Precursors》, and you may find the article in European Journal of Inorganic Chemistry.Category: imidazoles-derivatives The information in the text is summarized as follows:

The 4,4′-dimethylenebiphenyl linked sym. bis-(2-chlorobenzimidazole) (1) and the unsym. 2-chlorobenzimidazolium/2-chlorobenzimidazole [2(BF4)] have been reacted with one equiv of [Pd(PPh3)4] in oxidative addition reactions. For the sym. bis-NHC precursor 1, double metalation of both 2-chlorobenzimidazole sites to give the dinuclear bis-pNHC complex ([3][BF4]2) was observed The unsym. compound 2(BF4) was only metalated at the 2-chlorobenzimidazolium site with formation of the mononuclear NHC complex ([4][BF4]). The remaining 2-chlorobenzimidazole moiety was subsequently metalated in a second oxidative addition reaction with [M(PPh3)4] (M = Pd, Pt) to give the homobimetallic NHC/pNHC complex [5](BF4)2 (M = Pd) and the heterobimetallic complex [6](BF4)2 demonstrating the unique site-selective metalation of the bis-NHC precursor 2(BF4) by two consecutive oxidative additions After reading the article, we found that the author used 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

The author of 《Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903》 were Sharma, Swagat H.; Pablo, Juan Lorenzo; Montesinos, Monica Suarez; Greka, Anna; Hopkins, Corey R.. And the article was published in Bioorganic & Medicinal Chemistry Letters in 2019. Safety of 2-Chloro-1H-benzo[d]imidazole The author mentioned the following in the article:

The transient receptor potential cation channel 5 (TRPC5) has been previously shown to affect podocyte survival in the kidney. As such, inhibitors of TRPC5 are interesting candidates for the treatment of chronic kidney disease (CKD). Herein, we report the synthesis and biol. characterization of a series of N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors. Work reported here evaluates the benzimidazole scaffold and substituents resulting in the discovery of I, a TRPC5 inhibitor that is active in multiple animal models of CKD. The results came from multiple reactions, including the reaction of 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Safety of 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.Safety of 2-Chloro-1H-benzo[d]imidazole

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