Syntesis of thio- and seleno-acetamides bearing benzenesulfonamide as potent inhibitors of human carbonic anhydrase II and XII |
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| Institution: | 1. University of Florence, Department of Chemistry “Ugo Schiff”, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, Italy;2. University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;1. Department of Marine Life Sciences, Jeju National University, Jeju 63243, Republic of Korea;2. Department of Biological Sciences, Faculty of Applied Science, University of Rajarata, Mihintale 50300, Sri Lanka;3. Department of Molecular Biology, College of Natural Sciences and Human Ecology, Dongeui University, Busan 67340, Republic of Korea;4. Department of Biochemistry, College of Oriental Medicine, Dong-Eui University, Busan 47227, Republic of Korea;5. Department of Biology Education, Daegu University, Jillyang, Gyeongsan, Gyeonsangbuk-do 38453, Republic of Korea;6. Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Chungcheongbuk-do 28116, Republic of Korea;1. University of Florence, Department of Chemistry “Ugo Schiff”, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino, Italy;2. University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;1. Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;2. Department of Biological Sciences and Chemistry, University of Nizwa, Birkat Al-Mauz, P.O.Box 33, Nizwa 616, Oman;3. Istituto di Bioscienze e Biorisorse, CNR, Via Pietro Castellino 111, 80131 Napoli, Italy;1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Eini Street, 11562, Cairo, Egypt;2. University of Florence, Neurofarba Department, Via Ugo Schiff 6, Polo Scientifico, 50019, Sesto Fiorentino, Firenze, Italy;3. Yildirim Beyazit University Faculty of Medicine, Department of Medical Biology, Cinnah Campus, Ankara, Turkey |
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| Abstract: | A novel series of thio- and seleno-acetamides bearing benzenesulfonamide were synthetized and tested as human carbonic anhydrase inhibitors. These compounds were tested for the inhibition of four human (h) isoforms, hCA I, II, IX, and XII, involved in pathologies such as glaucoma (CA II and XII) or cancer (CA IX/XII). Several derivatives showed potent inhibition activity in low nanomolar range such as 3a, 4a, 7a and 8a. Furthermore, based on the tail approach we explain the interesting and selective inhibition profile of compound such as 5a and 9a, which were more selective for hCA I, 9b which was selective for hCA II, 3f selective for hCA IX and finally, 3e and 4b selective for hCA XII, over the other three isoforms. They are interesting leads for the development of more effective and isoform-selective inhibitors. |
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| Keywords: | Carbonic anhydrases (CAs) Carbonic anhydrase inhibitors (CAIs) Selenium Metalloenzymes Organoselenium compounds |
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