Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors.

Clicks: 346
ID: 58201
2019
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Abstract
Two new series of 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives containing either five membered heterocyclic rings or aryl hydrazones were synthesized and evaluated for their in vitro COX-1/COX-2 inhibitory activity. In vivo anti-inflammatory evaluation revealed that benzenesulfonamides bearing pyrazole moiety 19, 20 and its cyclized form 23 exhibited the highest anti-inflammatory activity with comparable potency to celecoxib. Furthermore, the ulcerogenic activity evaluation showed that compounds 19, 20 and 23 exerted the minimal ulcer index in comparison to indomethacin as a reference drug. Docking studies of the most selective COX-2 derivatives were also carried out against COX-2 active site. Benzenesulfonamide derivatives 19 and 20 displayed higher predicted binding affinities inside the COX-2 active site. Molecular modelling simulation and drug likeness studies showed good agreement with the obtained biological evaluation.
Reference Key
taher2019noveleuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Taher, Ehab S;Ibrahim, Tarek S;Fares, Mohamed;Al-Mahmoudy, Amany M M;Radwan, Abdullah F;Orabi, Khaled Y;El-Sabbagh, Osama I;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30260-0
URL
Keywords
anti-inflammatory benzenesulfonamide cox-2 benzisothiazol celecoxib saccharin

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