N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II
BIOORGANIC & MEDICINAL CHEMISTRY, cilt.23, sa.10, ss.2598-2605, 2015 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 23 Sayı: 10
- Basım Tarihi: 2015
- Doi Numarası: 10.1016/j.bmc.2014.12.054
- Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.2598-2605
- Anahtar Kelimeler: Sulfonamide, Imide, N-Acylsulfonamide, Carbonic anhydrase, Enzyme purification, Enzyme inhibition
- Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
- Atatürk Üniversitesi Adresli: Evet
Özet
Sulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 +/- 6.0-254.6 +/- 18.0 and 58.3 +/- 0.6-273.3 +/- 2.5 nM, respectively. (C) 2015 Elsevier Ltd. All rights reserved.