| Affiliation: | 1. NEUROFARBA Department, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy Department of Chemistry, COMSATS University Islamabad Abbottabad Campus, 22060 Abbottabad, Pakistan;2. NEUROFARBA Department, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy;3. Institute of Biosciences and Bioresources, CNR, Via Pietro Castellino 111, 80131 Napoli, Italy;4. Department of Chemistry, COMSATS University Islamabad Abbottabad Campus, 22060 Abbottabad, Pakistan |
| Abstract: | A series of benzylaminoethylureido-tailed benzenesulfonamides was analyzed for their inhibition potential against bacterial carbonic anhydrases (CAs) such as VhCA α, β, and γ from Vibrio cholerae, and BpsCA β and γ-CAs from Burkholderia pseudomallei. Growing drug resistance against antibiotics demands alternative targets and mechanisms of action. As CA is essential for the survival of bacteria, such enzymes have the potential for developing new antibiotics. Most of the compounds presented excellent inhibition potential against VhCA γ compared to α and β, with Ki values in the range of 82.5–191.4 nM. Several sulfonamides exhibited excellent inhibition against BpsCA β with Ki values in the range of 394–742.8 nM. Recently it has been demonstrated that sufonamide CA inhibitors are effective against vancomycin-resistant enterococci. These data show that CA inhibition of pathogenic bacteria may lead to a new class of antibiotics. |
