Inhibition Studies on Human and Mycobacterial Carbonic Anhydrases with N-((4-Sulfamoylphenyl)carbamothioyl) Amides.

ABSTRACT: A library of structurally diverse N-((4-sulfamoylphenyl)carbamothioyl) amides was synthesized by selective acylation of easily accessible 4-thioureidobenzenesulfonamide with various aliphatic, benzylic, vinylic and aromatic acyl chlorides under mild conditions. Inhibition of three α-class cytosolic human (h) carbonic anhydrases (CAs) (EC 4.2.1.1); that is, hCA I, hCA II and hCA VII and three bacterial β-CAs from Mycobacterium tuberculosis (MtCA1-MtCA3) with these sulfonamides was thereafter investigated in vitro and in silico. Many of the evaluated compounds displayed better inhibition against hCA I (K_I = 13.3-87.6 nM), hCA II (K_I = 5.3-384.3 nM), and hCA VII (K_I = 1.1-13.5 nM) compared with acetazolamide (AAZ) as the control drug (K_I

SUBMITTER: Abdoli M 

PROVIDER: S-EPMC10222120 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature