Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors.

ABSTRACT: We report here the synthesis and human carbonic anhydrases (CA, EC 4.2.1.1) inhibitory properties of a series of 4'-substituted 1,1'-biphenyl-4-sulfonamides incorporating a 2″- or 3″-amino- or carboxyphenyl unit. Most compounds showed significant variations in their inhibition profiles against CA II and IX when compared to previously reported analogs 12-18 bearing a 4″-amino or a 4″-carboxy group. In particular, compounds 1-11 showed considerable improvement of the CA II inhibitory efficacy with K _I values in the subnanomolar range (K _Is spanning between 0.57 and 31.0 nM), a drop of activity against CA IX (K _Is in the range 92.0 to 555.7 nM) and were as potent as 12-18 toward CA I (K

SUBMITTER: La Regina G 

PROVIDER: S-EPMC7236029 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature