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ABSTRACT:
SUBMITTER: Pichake J
PROVIDER: S-EPMC4094246 | biostudies-literature | 2014 Jul
REPOSITORIES: biostudies-literature
Pichake Jayashree J Kharkar Prashant S PS Ceruso Mariangela M Supuran Claudiu T CT Toraskar Mrunmayee P MP
ACS medicinal chemistry letters 20140516 7
A series of novel sulfonyl semicarbazides 5-13 was designed, synthesized, and evaluated for human carbonic anhydrase (hCA) inhibition. The new sulfonyl semicarbazides were tested against a panel of hCA isoforms I, II, IX, and XII, using acetazolamide (AZA, 1) as standard. All the sulfonyl semicarbazides showed subnanomolar affinity for hCA XII (pK i range 0.59-0.79 nM) and high selectivity over hCA I (58-114-fold) and hCA IX (26-114-fold) compared to hCA II (5-20-fold except 11, 121-fold). The i ...[more]