Tag: 255.1343

Chemical synthesis, molecular modeling and pharmacophore mapping of new pyrrole derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth was written by Joshi, Shrinivas D.;Kumar, S. R. Prem;Patil, Sonali;Vijayakumar, M.;Kulkarni, Venkatarao H.;Nadagouda, Mallikarjuna N.;Badiger, Aravind M.;Lherbet, Christian;Aminabhavi, Tejraj M.. And the article was included in Medicinal Chemistry Research in 2019.Safety of 2-Amino-4-(3-bromophenyl)thiazole This article mentions the following:

Abstract: Substituted phenylthiazolyl benzamide and pyrrolyl benzamide derivatives were developed using mol. hybridization technique to create novel lead antimycobacterial mols. used to fight against Mycobacteriumtuberculosis. The newly synthesized mols. have inhibited InhA, the enoyl-ACP reductase enzyme from the mycobacterial type II fatty acid biosynthetic pathway. Of these, compound 3b showed H-bonding interactions with Tyr158 and co-factor NAD⁺ that binds the active site of InhA. All the mols. were screened for in vitro antitubercular activity against M. tuberculosis H₃₇Rv, as well as some representative mols. as the inhibitors of InhA. Thirteen compounds exhibited good anti-TB activities (MIC = 1.6渭g/mL), but only few representative mols. showed the moderate InhA enzyme inhibition activity. [Figure not available: see fulltext.]. In the experiment, the researchers used many compounds, for example, 2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0Safety of 2-Amino-4-(3-bromophenyl)thiazole).

2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Safety of 2-Amino-4-(3-bromophenyl)thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies was written by Yan, Gang;Hao, Lina;Niu, Yan;Huang, Wenjie;Wang, Wei;Xu, Fengrong;Liang, Lei;Wang, Chao;Jin, Hongwei;Xu, Ping. And the article was included in European Journal of Medicinal Chemistry in 2017.SDS of cas: 105512-81-0 This article mentions the following:

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives, I (R¹ = Ph, 4-MeC₆H₄, 2-O₂NC₆H₄, etc.; R₂ = 2-MeOC₆H₄,3-MeOC₆H₄, 4-MeOC₆H₄, 3-EtOC₆H₄), II (R³ = Ph, 3,5-Cl₂-4-NH₂Ph; R⁴ = 3-MeOPh, 3-EtOPh), were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biol. evaluated in vitro. In addition, the selected compounds were tested with affinity (K_D) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog II (R³ = Ph; R⁴ = 3-EtOC₆H₄) (IC₅₀ = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization. In the experiment, the researchers used many compounds, for example, 2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0SDS of cas: 105512-81-0).

2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.SDS of cas: 105512-81-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Chemical synthesis, molecular modeling and pharmacophore mapping of new pyrrole derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth was written by Joshi, Shrinivas D.;Kumar, S. R. Prem;Patil, Sonali;Vijayakumar, M.;Kulkarni, Venkatarao H.;Nadagouda, Mallikarjuna N.;Badiger, Aravind M.;Lherbet, Christian;Aminabhavi, Tejraj M.. And the article was included in Medicinal Chemistry Research in 2019.Safety of 2-Amino-4-(3-bromophenyl)thiazole This article mentions the following:

Abstract: Substituted phenylthiazolyl benzamide and pyrrolyl benzamide derivatives were developed using mol. hybridization technique to create novel lead antimycobacterial mols. used to fight against Mycobacteriumtuberculosis. The newly synthesized mols. have inhibited InhA, the enoyl-ACP reductase enzyme from the mycobacterial type II fatty acid biosynthetic pathway. Of these, compound 3b showed H-bonding interactions with Tyr158 and co-factor NAD⁺ that binds the active site of InhA. All the mols. were screened for in vitro antitubercular activity against M. tuberculosis H₃₇Rv, as well as some representative mols. as the inhibitors of InhA. Thirteen compounds exhibited good anti-TB activities (MIC = 1.6μg/mL), but only few representative mols. showed the moderate InhA enzyme inhibition activity. [Figure not available: see fulltext.]. In the experiment, the researchers used many compounds, for example, 2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0Safety of 2-Amino-4-(3-bromophenyl)thiazole).

2-Amino-4-(3-bromophenyl)thiazole (cas: 105512-81-0) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Safety of 2-Amino-4-(3-bromophenyl)thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica