Document Detail

Synthesis and analgesic and anti-inflammatory activity of some new (6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid residues.
MedLine Citation:
PMID:  14502755     Owner:  NLM     Status:  MEDLINE    
In this study for developing potent analgesic and anti-inflammatory compounds, we synthesized 6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid side chain, and performed preliminary screening of their in vivo analgesic and anti-inflammatory activities at a single dose of 100 mg/kg inmice by a p-benzoquinone-induced writhing test and a Carrageenaninduced hind paw edema model, respectively. We also determined their gastric ulceration effects in the tested animals. Propanoic acid derivatives were generally found to have higher analgesic and anti-inflammatory activities, and among them, 3-(6-benzoyl-2-benzothiazolinon-3-yl)propanoic acid (Compound 4 a) exhibited the highest analgesic and anti-inflammatory activity. However, all compounds showed lower anti-inflammatory effects than we observed for indomethacin at 10 mg/kg dose. Consequently, 6-acyl-2-benzoxazolinone/2-benzothiazolinones having propanoic acid side chain might lead to further studies for developing better candidates with potent analgesic and anti-inflammatory effects while acetic acid derivatives do not exhibit comparable satisfactory features.
Serdar Unlü; Tijen Onkol; Yasemin Dündar; Berna Okçelik; Esra Küpeli; Erdem Yeşilada; Ningur Noyanalpan; M Fethi Sahin
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  336     ISSN:  0365-6233     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  2003 Aug 
Date Detail:
Created Date:  2003-09-22     Completed Date:  2003-11-03     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  353-61     Citation Subset:  IM    
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, 06330, Ankara, Turkey.
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MeSH Terms
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*,  pharmacology*
Edema / chemically induced,  prevention & control
Indicators and Reagents
Magnetic Resonance Spectroscopy
Pain Measurement / drug effects
Spectrophotometry, Infrared
Stomach Ulcer / chemically induced
Thiazoles / chemical synthesis,  pharmacology
Reg. No./Substance:
0/6-acyl-2-benzoxazolinone; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Indicators and Reagents; 0/Thiazoles

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