Substituted quinazolinones and their anti-inflammatory activity.
6-Substituted-2-alkyl-3-(4-aminobenzene sulphonamido)quinazolin-4-(3H) ones (1a-b) were converted either to 2-methyl 3-[(N-aminoacylbenzoate)benzenes sulphonamido]quinazolin-4 (3H) ones (2a-c) or to 6-substituted-2-alkyl-3-(N-arylidene benzene sulphonamido)-quinazolin-4- (3H) ones (3a-h). 3 on reduction, yielded 6-substituted-2-alkyl-3-(N-arylmethyl sulphonamido)-quinazolin-4(3H)ones (4a-l). Reaction of 3a-h with thioglycolic acid afforded 2-alkyl-3-[4'-(5'-arylthiazolidin-3'-one)benzene sulphonamido]quinazolin-4(3H)ones (5a-h). All these compounds were evaluated for their anti-inflammatory activity against carrageenin induced rat's paw oedema. Active compounds were also evaluated for ulcerogenic liability and ALD50 values.
Hitkari
A
A
Department of Pharmacology Therapeutics, K.G'S Medical College, Lucknow, India.
Bhalla
M
M
Saxena
A K
AK
Verma
M
M
Gupta
M P
MP
Shanker
K
K
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; 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
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011799:Quinazolines