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-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethylbenzamide (3d) and 2-hydroxymethyl-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-propylbenzamide (3e), respectively.
Okunrobo
Lucky O
LO
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, Nigeria.
Usifoh
Cyril O
CO
Scriba
Gerhard K E
GK
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D001894:Borohydrides / Q000737:chemistry; D002351:Carrageenan; D002384:Catalysis; D005260:Female; D007202:Indicators and Reagents; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D000432:Methanol; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D010797:Phthalimides / Q000138:chemical synthesis / Q000494:pharmacology; D011247:Pregnancy; D051381:Rats; D017208:Rats, Wistar; D012997:Solvents; D013055:Spectrophotometry, Infrared; D014867:Water
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001894:Borohydrides; D007202:Indicators and Reagents; D010797:Phthalimides; D012997:Solvents; D014867:Water; C025364:sodium borohydride; D002351:Carrageenan; D000432:Methanol