Yayınlanmış 1 Ocak 2016 | Sürüm v1
Dergi makalesi Açık

Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors

  • 1. Jamia Hamdard, Fac Sci, Dept Chem, New Delhi 110062, India
  • 2. Ondokuz Mayis Univ, Fac Agr, Dept Agr Biotechnol, TR-55139 Kurupelit, Turkey
  • 3. Ibrahim Cecen Univ Agri, Sci & Art Fac, Dept Chem, TR-04100 Agri, Turkey
  • 4. Univ Florence, Polo Sci, Lab Chim Bioinorgan, Rm 188,Via Lastruccia 3, I-50019 Florence, Italy

Açıklama

A series of sulfonamide derivatives (2a-l) incorporating substituted pyridazinone moieties were investigated for the inhibition of two human cytosolic carbonic anhydrase isoforms, hCA I and hCA II. All these compounds, together with the clinically used sulfonamide acetazolamide were investigated as inhibitors of the physiologically relevant isozymes I and II. These sulfonamides showed very strong inhibition against all these isoforms with K-I's in the range of 0.98-8.5 nM which makes such molecules possible to be used as leads for discovery of novel effective CA inhibitors targeting other isoforms with medicinal chemistry applications. (C) 2016 Elsevier Ltd. All rights reserved.

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