Biological investigation of N-methyl thiosemicarbazones as antimicrobial agents and bacterial carbonic anhydrases inhibitors |
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Authors: | Ilaria D’ Agostino,Githa Elizabeth Mathew,Paola Angelini,Roberto Venanzoni,Giancarlo Angeles Flores,Andrea Angeli,Simone Carradori,Beatrice Marinacci,Luigi Menghini,Mohamed A. Abdelgawad,Mohammed M. Ghoneim,Bijo Mathew,Claudiu T. Supuran |
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Abstract: | The enormous burden of the COVID-19 pandemic in economic and healthcare terms has cast a shadow on the serious threat of antimicrobial resistance, increasing the inappropriate use of antibiotics and shifting the focus of drug discovery programmes from antibacterial and antifungal fields. Thus, there is a pressing need for new antimicrobials involving innovative modes of action (MoAs) to avoid cross-resistance rise. Thiosemicarbazones (TSCs) stand out due to their easy preparation and polypharmacological application, also in infectious diseases. Recently, we reported a small library of TSCs (1–9) that emerged for their non-cytotoxic behaviour. Inspired by their multifaceted activity, we investigated the antibacterial, antifungal, and antidermatophytal profiles of derivatives 1–9, highlighting a new promising research line. Furthermore, the ability of these compounds to inhibit selected microbial and human carbonic anhydrases (CAs) was assessed, revealing their possible involvement in the MoA and a good selectivity index for some derivatives. |
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Keywords: | Thiosemicarbazones antimicrobial agents Escherichia coli dermatophytes carbonic anhydrases |
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