Journal of enzyme inhibition and medicinal chemistry · 2022
Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae.
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Giovannuzzi Simone, Abutaleb Nader S, Hewitt Chad S, Carta Fabrizio, Nocentini Alessio, Seleem Mohamed N, Flaherty Daniel P, Supuran Claudiu T
Аннотация
Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the α-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. KIs 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 µg/mL. As NgCA was recently validated as an antibacterial drug target, the DTCs may lead to development of novel antigonococcal agents.