Aniline Derivatives as Potent Carbonic Anhydrase Inhibitors
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| Year of publication | 2025 |
| Type | Appeared in Conference without Proceedings |
| MU Faculty or unit | |
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| Description | Carbonic anhydrases are omnipresent metalloenzymes that catalyze reversible conversion of carbon dioxide to bicarbonate and proton, maintaining homeostasis. In humans, they are involved in multiple physiological processes, and they are linked to many disorders, such as glaucoma, neurodegeneration or cancer. Their potential inhibition is of considerable interest in biomedical research. [1]. In bacteria, inhibition of carbonic anhydrases leads to inhibition of their growth and makes them more vulnerable to host defense mechanisms [2]. Based on our previous findings, where a lead 1,3,5-triazinyl aminobenzenesulfonamide incorporating an aniline motif exhibited high inhibitory activity against carbonic anhydrase (K? = 7.4 nM against CA IX ), we designed and synthesized a series of related derivatives to further explore structure–activity relationships and improve selectivity. The new compounds were evaluated for their inhibitory activity against various CA isoforms. |
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