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Synthesis and Biological Evaluation of New Diarylpyrazole and Triarylimidazoline Derivatives as Selective COX‐2 Inhibitors
Author(s) -
Abdellatif Khaled R.A.,
Abdelgawad Mohamed A.,
Labib Madlen B.,
Zidan Taha H.
Publication year - 2017
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201600386
Subject(s) - celecoxib , in vivo , chemistry , cyclooxygenase , selectivity , in vitro , pharmacology , stereochemistry , biological activity , chemical synthesis , enzyme , biochemistry , catalysis , biology , microbiology and biotechnology
New series of diarylpyrazoles 8a–f and triarylimidazoline‐5‐ones 11a–g were synthesized and evaluated for their in vitro cyclooxygenase‐1 (COX‐1) and COX‐2 inhibitory activity and in vivo anti‐inflammatory activity. The synthesized compounds showed good selectivity for COX‐2; compounds 8a , 8d , 8f , 11a , and 11c exhibited the highest COX‐2 selectivity indexes (SI = 4.77–5.43) compared to the reference drug celecoxib (SI = 7.8). All compounds showed good in vivo anti‐inflammatory activity, especially compounds 8a , 8f , 11c , and 11d , which also showed some similarities to the time interval pattern of celecoxib at all different time intervals (1, 3, and 6 h).