Meng, Fanfei; Mi, Pengcheng; Yu, Zhenwu; Wei, Wei; Gao, Li; Ren, Jinzhou; Li, Zhengming; Dai, Huanqin published the artcile< Design, synthesis and biological evaluation of 5-substituted sulfonylureas as antifungal agents targeting acetohydroxyacid synthase>, Recommanded Product: o-Chlorobenzenesulfonamide, the main research area is sulfonylurea preparation antifungal.
In this work, 36 target compounds I were designed and synthesized and several 5-substituted sulfonylureas I = [X =CH, N, R1 = Me, Cl, Br; R2 = CNOMe, CHCH2, CHO; R3 = H, Me, OMe; R4 = Me, OMe, etc.] possess much better antifungal activities than those of Fluconazole (FCZ) and amphotericin B (AMB). The most potent of these were I [X =CH, R1 = Br, R2 = CNOMe, R3 = R4 = OCH3], I [X =CH, R1 = Cl, R2 = CHCH2, R3 = R4 = OCH3] and I [X =CH, R1 = I, R2 = CHCH2, R3 = R4 = OCH3] with inhibition constants (Ki) determined in the range of 5.6∼9.6 nM for C. albicans AHAS and MICs(The MIC was determined as the drug concentration that inhibited fungal growth by >90% relative to the corresponding drug-free growth control) <0.05∼0.78μg/mL for C. albicans SC 5314, 17# and 2# (17# and 2# were two clin. isolated FCZ-resistant strains of C. albicans), S. cerevisiae SCXH1549 and C. parapsilosis ATCC22019 in YNB (yeast nitrogen base) media at 72 h post-treatment. Using the same media, the com. MICs of FCZ and AMB were only determined in the range of 0.25∼5μg/mL for the five strains at 24 h post-treatment. In order to elaborate the structure-activity relationship (SAR) a proposed double-pocket binding mode was simulated via mol. docking. The energy gap between the HOMOs and LUMOs of selected compounds showed that the 5-substituted groups of sulfonylureas I = [X =CH, N, R1 = Me, Cl, Br; R2 = CNOMe, CHCH2, CHO; R3 = H, Me, OMe; R4 = Me, OMe, etc.] had key impact on the antimicrobial bioactivity. Journal of Molecular Structure published new progress about Fungicides. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Recommanded Product: o-Chlorobenzenesulfonamide.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics