In:
Archiv der Pharmazie, Wiley, Vol. 349, No. 10 ( 2016-10), p. 801-807
Abstract:
A new series of 1,3,5‐triarylpyrazolines 13a–l was synthesized and all prepared compounds were evaluated for their in vitro COX‐1/COX‐2 inhibitory activity and in vivo anti‐inflammatory activity. All test compounds were more selective for the COX‐2 isozyme and showed good in vivo anti‐inflammatory activity. Compound 13h was the most COX‐2 selective compound (COX‐2 selectivity index (SI) = 10.23) and the most potent anti‐inflammatory derivative (ED 50 = 60.1 µmol/kg) in comparison with celecoxib (COX‐2 SI = 9.29 and ED 50 = 81.4 µmol/kg). All screened compounds were less ulcerogenic (ulcer indexes (UI) = 0.33–1.33) than aspirin (UI = 2.33) and comparable to celecoxib (UI = 0.33).
Type of Medium:
Online Resource
ISSN:
0365-6233
,
1521-4184
DOI:
10.1002/ardp.v349.10
DOI:
10.1002/ardp.201600145
Language:
English
Publisher:
Wiley
Publication Date:
2016
detail.hit.zdb_id:
1496815-0
SSG:
15,3
