Synthesis and anti-inflammatory activity of some new 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazole derivatives

A series of 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazoles were designed and synthesized in order to obtain new compounds with potential anti-inflammatory activity. The title compounds were screened for in vivo anti-inflammatory activity by using Carrageenan induced rat paw edema meth...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (21), p.6527-6532
Hauptverfasser: Dekhane, Deepak V, Pawar, Shivaji S, Gupta, Sunil, Shingare, Murlidhar S, Patil, C.R, Thore, Shivaji N
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Sprache:eng
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Zusammenfassung:A series of 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazoles were designed and synthesized in order to obtain new compounds with potential anti-inflammatory activity. The title compounds were screened for in vivo anti-inflammatory activity by using Carrageenan induced rat paw edema method. Diclofenac sodium was used as a standard drug for comparison. Out of the 30 compounds tested, compound 19a, 19b, 25a, 25b exhibited significant anti-inflammatory activity. Selected compounds were also screened for in vitro COX-2 inhibition assay and analgesic activity in the acetic acid induced writhing model.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.08.061