Synthesis and pharmacological evaluation of 2-hydroxymethylbenzamides as anti-inflammatory and analgesic agents

The ring opening of some phthalimide derivatives with sodium borohydride in methanol/water (6:1) afforded the corresponding 2-hydroxymethylbenzamides irrespective of the substituents. The most active members of the series evaluated for anti-inflammatory and analgesic activities were 2-hydroxymethyl-...

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Veröffentlicht in:	Acta Poloniae pharmaceutica 2006-01, Vol.63 (1), p.25-31
Hauptverfasser:	Okunrobo, Lucky O, Usifoh, Cyril O, Scriba, Gerhard K E
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics - chemical synthesis Analgesics - pharmacology Animals Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - pharmacology Borohydrides - chemistry Carrageenan Catalysis Female Indicators and Reagents Inflammation - chemically induced Inflammation - drug therapy Magnetic Resonance Spectroscopy Male Methanol Mice Pain Measurement - drug effects Phthalimides - chemical synthesis Phthalimides - pharmacology Pregnancy Rats Rats, Wistar Solvents Spectrophotometry, Infrared Water
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Zusammenfassung:	The ring opening of some phthalimide derivatives with sodium borohydride in methanol/water (6:1) afforded the corresponding 2-hydroxymethylbenzamides irrespective of the substituents. The most active members of the series evaluated for anti-inflammatory and analgesic activities were 2-hydroxymethyl-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethylbenzamide (3d) and 2-hydroxymethyl-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-propylbenzamide (3e), respectively.
ISSN:	0001-6837