Giovannuzzi, SimoneAbutaleb, Nader S.Hewitt, Chad S.Carta, FabrizioNocentini, AlessioSeleem, Mohamed N.Flaherty, Daniel P.Supuran, Claudiu T.2022-08-242022-08-242022-01-011475-6366http://hdl.handle.net/10919/111622Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the alpha-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae, NgCA. As an extension to our previous studies, we report that dithiocarbamates (DTCs) derived from primary or secondary amines constitute a class of efficient inhibitors of NgCA. K(I)s ranging between 83.7 and 827 nM were measured for a series of 31 DTCs that incorporated various aliphatic, aromatic, and heterocyclic scaffolds. A subset of DTCs were selected for antimicrobial testing against N. gonorrhoeae, and three molecules displayed minimum inhibitory concentration (MIC) values less than or equal to 8 mu g/mL. As NgCA was recently validated as an antibacterial drug target, the DTCs may lead to development of novel antigonococcal agents.application/pdfenCreative Commons Attribution 4.0 InternationalCarbonic anhydraseinhibitordithiocarbamateNeisseria gonorrhoeaeantibacterialsArticle - Refereedhttps://doi.org/10.1080/14756366.2021.1988945371348949541475-6374