Anti-inflammatory and analgesic activity of indolyl quinazolones and their congeners.
6,8-Disubstituted-2-methyl-3-[2-substituted-indol-3-yl-methyl(ene)imino] -quinazoline-4(3H)-ones (III), 6,8-disbustituted-2-methyl-3-[2-substituted-indol-3-yl methyl amino]-quinazoline-4(3H)-ones (IV), 6,8-disubstituted-2-methyl-2-[5-(2-substituted-indol-3-yl)-thiazolidine- 3- one]quinazoline-4(3H)-ones (V), propionic acid derivative of 6,8-disubstituted-2-methyl-3-[5-(2-substituted indol-3-yl)-thiazolidine-3-one]-quinazoline-4(3H)-ones (VI), 6,8-disubstituted-2-methyl-3-[5-(2-substituted-indol-3-yl)-2-substituted benzylidine-thiazolidine-3-one]-quinazoline 4(3H)-ones (VII), 6,8-disubstituted-2-methyl-3-[2-substituted-indol-3-yl-4- chloroazetidine-1-one]-quinazoline-4-(3H)-ones (VIII), and 6,8-disubstituted-2-methyl-3-[2-substituted-indol-3- yl-alpha-arylazo methylimino]-quinazoline-4(3H)-ones (IX) were synthesized and evaluated for their anti-inflammatory activity against carrageenin induced paw oedema. The compounds found potent were further tested for their anti-writhmogenic activity in albino mice. The compounds exhibiting significant anti-inflammatory activity also showed marked protection against aconitine induced writhing response. The low toxicity of the potent compounds was also reflected by their high approximate LD50 values.
Bhalla
M
M
Department of Pharmacology and Therapeutics, King George's Medical College, Lucknow, India.
Srivastava
V K
VK
Bhalla
T N
TN
Shanker
K
K
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D011799:Quinazolines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007211:Indoles; D011799:Quinazolines; D002351:Carrageenan