Structure-analgesic activity relationships in a set of 2-aminobenzamide derivatives.
A set of 2-aminobenzamide derivatives designed as analgesic following the principles of correlation analysis have been prepared and tested. The analgesic effects shown by these products are similar to those of non-narcotic analgesic drugs; moreover, they do not show antipyretic effects and are inactive or very poor inhibitors of prostaglandin synthesis. Quantitative structure-activity relationships (QSAR) show that the analgesic potency (writhing test) is a function of the octanol-water partition coefficient. The predictive value of a correlation equation previously published is clearly demonstrated.
R
R
Lisciani
S
S
Lembo
S
S
Cozzolino
M I
MI
La Rotonda
C
C
Silipo
A
A
Vittoria
D000082:Acetaminophen / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000983:Antipyrine / Q000494:pharmacology; D001241:Aspirin / Q000494:pharmacology; D001341:Autonomic Nervous System / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D003061:Codeine / Q000494:pharmacology; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D011453:Prostaglandins / Q000096:biosynthesis; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000700:Analgesics; D011453:Prostaglandins; D062367:ortho-Aminobenzoates; D000082:Acetaminophen; D009020:Morphine; D001241:Aspirin; D000983:Antipyrine; D003061:Codeine