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Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae.

ABSTRACT: 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.

SUBMITTER: Giovannuzzi S 

PROVIDER: S-EPMC8667944 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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Dithiocarbamates effectively inhibit the α-carbonic anhydrase from <i>Neisseria gonorrhoeae</i>.

Giovannuzzi Simone S   Abutaleb Nader S NS   Hewitt Chad S CS   Carta Fabrizio F   Nocentini Alessio A   Seleem Mohamed N MN   Flaherty Daniel P DP   Supuran Claudiu T CT  

Journal of enzyme inhibition and medicinal chemistry 20221201 1

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 <i>Neisseria gonorrhoeae</i>, 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<sub>I</sub>s ranging between 83.7 and 827 nM were measured for a series of 3  ...[more]

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