Premium
Synthesis and Biological Evaluation of Some Hydroxypyrazole Derivatives as Anti‐inflammatory‐Antimicrobial Agents
Author(s) -
Bekhit Adnan A.,
AbdelRahman Hamdy M.,
Guemei Aida A.
Publication year - 2006
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.200500197
Subject(s) - antimicrobial , chemistry , trifluoroacetic anhydride , acetic anhydride , acylation , organic chemistry , catalysis
Some hydroxypyrazole derivatives 2 – 7 were synthesized by cyclocondensation of the keto‐ester 1 with hydrazines hydrate or substituted hydrazines followed by reduction and acylation with acetic anhydride or trifluoroacetic anhydride. The newly synthesized compounds were evaluated for their anti‐inflammatory, antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined. Compounds N ‐(4‐(5‐hydroxy‐1‐trifluoroacetyl‐1 H ‐pyrazol‐3‐yl)phenyl) trifluoroacetamide 4b , 3‐(4‐nitrophenyl)‐1‐(4‐methoxyphenyl)‐1 H ‐pyrazol‐5‐ol 5b , and N ‐(4‐(5‐hydroxy‐1‐methyl‐1 H ‐pyrazol‐3‐yl)phenyl)trifluoroacetamide 7b were proved to be the most active anti‐inflammatory, antimicrobial agents in the present study with a good safety margin and minimal or no ulcerogenic effect.