Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents was written by Zhao, Liyu;Sun, Yin;Yin, Wenbo;Tian, Linfeng;Sun, Nannan;Zheng, Yang;Zhang, Chu;Zhao, Shizhen;Su, Xin;Zhao, Dongmei;Cheng, Maosheng. And the article was included in European Journal of Medicinal Chemistry in 2022.Application of 7312-11-0 This article mentions the following:
To discover antifungal compounds with broad-spectrum and stable metabolism, a series of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives were designed and synthesized. Compounds I [R1 = 6-F, 6-Cl, 6-Br; R2 = 4-F] and [R1 = 6-Cl, 6-Br; R2 = 4-Cl] exhibited excellent broad-spectrum antifungal activity against Candida albicans with MIC values in the range of 0.03-0.5μg/mL, and against Cryptococcus neoformans and Aspergillus fumigatus with MIC values in the range of 0.25-2μg/mL. In addition, compounds I [R1 = 6-Cl; R2 = 4-F] and [R1 = 6-Cl; R2 = 4-Cl] showed high metabolic stability in human liver microsomes in vitro, with the half-life of 80.5 min and 69.4 min, resp. Moreover, compounds I [R1 = 6-Cl; R2 = 4-F] and [R1 = 6-Cl; R2 = 4-Cl] showed weak or almost no inhibitory effect on the CYP3A4 and CYP2D6. The pharmacokinetic evaluation in SD rats showed that compoundI [R1 = 6-Cl; R2 = 4-F] had suitable pharmacokinetic properties and was worthy of further study. In the experiment, the researchers used many compounds, for example, Methyl 5-bromobenzo[b]thiophene-2-carboxylate (cas: 7312-11-0Application of 7312-11-0).
Methyl 5-bromobenzo[b]thiophene-2-carboxylate (cas: 7312-11-0) belongs to benzothiophene derivatives. Functionalized benzothiophenes are important constructs found in molecules with wide ranging biological activity and in organic materials. It is found within the chemical structures of pharmaceutical drugs such as zileuton, raloxifene, and sertaconazole, and also BTCP.Application of 7312-11-0
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem