Synthesis and Biological Evaluation of Some Hydroxypyrazole Derivatives as Anti-inflammatory-Antimicrobial Agents

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‐infla...

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Bibliographic Details
Published in:Archiv der Pharmazie (Weinheim) 2006-02, Vol.339 (2), p.81-87
Main Authors: Bekhit, Adnan A., Abdel-Rahman, Hamdy M., Guemei, Aida A.
Format: Article
Language:English
Subjects:
Acute Toxicity
Animals
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - pharmacology
Anti-Infective Agents - toxicity
Anti-inflammatory
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - pharmacology
Anti-Inflammatory Agents - toxicity
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimicrobial
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
General aspects
Hydroxypyrazole
Male
Medical sciences
Mice
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - pharmacology
Pyrazoles - toxicity
Rats
Rats, Sprague-Dawley
Stomach Ulcer - chemically induced
Ulcerogenic effect
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Summary: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‐1H‐pyrazol‐3‐yl)phenyl) trifluoroacetamide 4b, 3‐(4‐nitrophenyl)‐1‐(4‐methoxyphenyl)‐1H‐pyrazol‐5‐ol 5b, and N‐(4‐(5‐hydroxy‐1‐methyl‐1H‐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.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.200500197