title: Synthesis of 3-(2-pyridyl)-2-substituted-quinazolin-4(3H)-ones as new analgesic and anti-inflammatory agents.
abstract: A new series of 3-(2-pyridyl)-2-substituted-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 2-hydrazino-3-(2-pyridyl)-quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(2-pyridyl)-quinazolin-4(3H)-one was synthesized from 2-aminopyridine. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. While the test compounds exhibited significant activity, compound 2-(1-ethylpropylidene)-hydrazino-3-(2-pyridyl)-quinazolin-4(3H)-one (AS2) showed moderate analgesic activity and compound 2-(1-methylbutylidene)-hydrazino-3-(2-pyridyl)-quinazolin-4(3H)-one (AS3) showed realistic anti-inflammatory activity when compared to the reference standard diclofenac sodium. Interestingly the test compounds showed only mild ulcerogenic side effect when compared to aspirin.
authors.affiliation: Medicinal Chemistry R&D Laboratory, Arulmigu Kalasalingam College of Pharmacy, Anand Nagar, Krishnankovil, Tamil Nadu-626 190, India. drvalagarsamy@gmail.com
authors.forename: V
authors.initials: V
authors.lastname: Alagarsamy
authors.forename: V Raja
authors.initials: VR
authors.lastname: Solomon
authors.forename: M
authors.initials: M
authors.lastname: Murugan
authors.forename: R
authors.initials: R
authors.lastname: Sankaranarayanan
authors.forename: P
authors.initials: P
authors.lastname: Periyasamy
authors.forename: R
authors.initials: R
authors.lastname: Deepa
authors.forename: T Durai
authors.initials: TD
authors.lastname: Anandkumar
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D012015:Reference Standards; D013055:Spectrophotometry, Infrared; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D007202:Indicators and Reagents; D011725:Pyridines; D052999:Quinazolinones; D002351:Carrageenan