Antiinflammatory and antinociceptive activities of some benzotriazolylalkanoic acids.
Sets of benzotriazol-1/2-ylalkanoic acids (1, 2, 3) and benzotriazol-1-yloxyalkanoic acids (4, 5) were prepared and tested for antiinflammatory activity; when significant activity was observed also the antinociceptive activity was explored. While the acids of structure 1, 4 and 5 were devoid of antiinflammatory action, most 2-(benzotriazol-1/2-yl)propionic acids (2, 3) exhibited significant activity as antiinflammatory and antinociceptive agents, with compound 2c and 3a being the most active in the two assays, respectively. The dextrorotatory enantiomer of 2c ((+)-2c) was also prepared and found to be practically as active as the racemic mixture, though some differences in the steepness of the dose-response curves were observed.
Boido
Alessandro
A
Dipartimento di Scienze Farmaceutiche, Università di Genova, Italy.
Vazzana
Iana
I
Mattioli
Francesca
F
Sparatore
Fabio
F
D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology*
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D014230:Triazoles; C012771:benzotriazole