| Literature DB >> 27253845 |
Daniela Vullo1, Mariaconcetta Durante2, Francesco Saverio Di Leva3, Sandro Cosconati4, Emanuela Masini2, Andrea Scozzafava1, Ettore Novellino3, Claudiu T Supuran1,5, Fabrizio Carta1.
Abstract
A series of monothiocarbamates (MTCs) were prepared from primary/secondary amines and COS as potential carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, using the dithiocarbamates, the xanthates, and the trithiocarbonates as lead compounds. The MTCs effectively inhibited the pharmacologically relevant human (h) hCAs isoforms I, II, IX, and XII in vitro and showed KIs spanning between the low and medium nanomolar range. By means of a computational study, the MTC moiety binding mode on the CAs was explained. Furthermore, a selection of MTCs were evaluated in a normotensive glaucoma rabbit model for their intraocular pressure (IOP) lowering effects and showed interesting activity.Entities:
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Year: 2016 PMID： 27253845 DOI： 10.1021/acs.jmedchem.6b00462
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446