Synthesis and pharmacological evaluation of some 3-(4-methylphenyl)-2-substituted amino-3H-quinazolin-4-ones as analgesic and anti-inflammatory agents.
A variety of 3-(4-methyl phenyl)-2-substituted amino-3H-quinazolin-4-ones were synthesized by reacting the amino group of 2-hydrazino-3-(4-methyl phenyl)-3H-quinazolin-4-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(4-methyl phenyl)-3H-quinazolin-4-one was synthesized from 4-methyl aniline. The title compounds were investigated for analgesic, anti-inflammatory, and ulcerogenic index activities. While the test compounds exhibited significant activity, compounds Al, A2, and A3 showed more potent analgesic activity and the compound A3 showed more potent anti-inflammatory activity when compared to the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared to aspirin.
Alagarsamy
Veerachamy
V
Medicinal Chemistry Research Laboratory, Arulmigu Kalasalingam College of Pharmacy, Anand Nagar, Krishnankovil, India. samy_veera@yahoo.com
Shankar
Durairaj
D
Murugan
Muthuvel
M
Siddiqui
Anees Ahmed
AA
Rajesh
Ramadoss
R
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001241:Aspirin / Q000633:toxicity; D002351:Carrageenan; D004008:Diclofenac / Q000494:pharmacology; D004195:Disease Models, Animal; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010147:Pain Measurement; D017288:Pain Threshold / Q000187:drug effects; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D052999:Quinazolinones; D004008:Diclofenac; D002351:Carrageenan; D001241:Aspirin