1. Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides
- Author
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Claudiu T. Supuran, Murat Şentürk, Tayfun Arslan, Emir Alper Türkoğlu, Fakülteler, Fen - Edebiyat Fakültesi, Kimya Bölümü, Arslan, Tayfun, and Belirlenecek
- Subjects
Gene isoform ,Chalcone ,Carbonic Anhydrase I ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Inhibitory postsynaptic potential ,01 natural sciences ,Biochemistry ,Clinical biochemistry ,Carbonic Anhydrase II ,Catalysis ,Carbonic Anhydrase ,chemistry.chemical_compound ,Structure-Activity Relationship ,Carbonic anhydrase ,Drug Discovery ,Humans ,Carbonic Anhydrase Inhibitors ,Molecular Biology ,chemistry.chemical_classification ,Sulfonamides ,biology ,Dose-Response Relationship, Drug ,Molecular Structure ,Inhibitors ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,0104 chemical sciences ,Sulfonamide ,010404 medicinal & biomolecular chemistry ,biology.protein ,Molecular Medicine - Abstract
Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes involved in many bioprocesses, through catalysis of the reversible hydration/dehydration process of CO2/HCO3-. The inhibition of human CA isoforms I and II with a new series of sulfonamide derivatives incorporating substituted chalcone moieties were studied in this study. All these newly synthesized sulfonamides demonstrated important inhibitory profiles to these CA isoforms with K(1)s in the range of 9.88 to 55.43 nM, making these compounds interesting leads, with potential applications in medicinal chemistry. (C) 2016 Published by Elsevier Ltd., Scientific and Technical Research Council of Turkey (TUBITAK) [KBAG-115Z078], We are greatly indebted to The Scientific and Technical Research Council of Turkey (TUBITAK, Grant No. KBAG-115Z078) for their financial support for this work.
- Published
- 2016