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DOI 10.1016/j.bioorg.2019.103153

Медицинская библиотека · Bioorganic chemistry · 2019

Synthesis, molecular docking analysis and carbonic anhydrase I-II inhibitory evaluation of new sulfonamide derivatives.

Sağlık Begüm Nurpelin, Çevik Ulviye Acar, Osmaniye Derya, Levent Serkan, Çavuşoğlu Betul Kaya, Demir Yeliz, Ilgın Sinem, Özkay Yusuf, Koparal Ali Savaş, Beydemir Şükrü, Kaplancıklı Zafer Asım

Оценочное исследованиеСтатьяПоддержка исследования: вне правительства СШАПеревод в очереди

Аннотация

New sulfonamide-hydrazone derivatives (3a-3n) were synthesized to evaluate their inhibitory effects on purified human carbonic anhydrase (hCA) I and II. The inhibition profiles of the synthesized compounds on hCA I-II isoenzyme were investigated by comparing their IC50 and Ki values. Acetazolamide (5-acetamido-1,3,4-thiadiazole-2-sulfonamide, AZA) has also been used as a standard inhibitor. The compound 3e demonstrated the best hCA I inhibitory effect with a Ki value of 0.1676 ± 0.017 µM. Besides, the compound 3m showed the best hCA II inhibitory effect with a Ki value of 0.2880 ± 0.080 µM. Cytotoxicity of the compounds 3e and 3m toward NIH/3T3 mouse embryonic fibroblast cell line was observed and the compounds were found to be non-cytotoxic. Molecular docking studies were performed to investigate the interaction types between active compounds and hCA enzymes. Pharmacokinetic profiles of compounds were assessed by theoretical ADME predictions. As a result of this study a novel and potent class of CA inhibitors were identified with a good activity potential.

Для цитирования: Sağlık Begüm Nurpelin, Çevik Ulviye Acar, Osmaniye Derya, Levent Serkan, Çavuşoğlu Betul Kaya, Demir Yeliz, Ilgın Sinem, Özkay Yusuf, Koparal Ali Savaş, Beydemir Şükrü, Kaplancıklı Zafer Asım. Synthesis, molecular docking analysis and carbonic anhydrase I-II inhibitory evaluation of new sulfonamide derivatives.. Bioorganic chemistry. 2019. DOI: 10.1016/j.bioorg.2019.103153.

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