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KMID : 0043320150380111932
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Archives of Pharmacal Research
2015 Volume.38 No. 11 p.1932 ~ p.1942
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Synthesis and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing an aminosulphonyl pharmacophore
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Abdellatif Khaled R. A.
Abdelgawad Mohamed A.
Elshemy Heba A. H.
Alsayed Shahinda S. R.
Kamel Gehan
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Abstract
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A novel series of 2-pyrazoline derivatives 13a?l was synthesized via aldol condensation of 4-substituted acetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-hydrazinobenzenesulfonamide hydrochloride. The chemical structures of the target pyrazoline derivatives were proved by means of IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses data. All the synthesized compounds were evaluated for their cyclooxygenase selectivity, anti-inflammatory and ulcerogenic liability. While compounds 13e, 13h and 13i showed moderate COX-2 selectivity in vitro and good anti-inflammatory activity in vivo, compound 13i showed the highest anti-inflammatory activity that is very close in potency to the reference drug (celecoxib) with better gastric profile than celecoxib.
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KEYWORD
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Dihydropyrazole, Cyclooxygenase inhibition, Anti-inflammatory
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