title: Synthesis of 4-substituted pyrido[2,3-d]pyrimidin-4(1H)-one as analgesic and anti-inflammatory agents.
abstract: 4-Substituted-pyrido[2,3-d]pyrimidin-4(1H)-ones 4a-c were synthesized by oxidation of 4-substituted-dihydropyrido[2,3-d]pyrimidin-4(1H)-ones 3a-c which were in turn prepared from arylidenemalononitriles 1a-c and 6-aminothiouracil 2. The reactivity of compounds 4a-c towards some reagents such as formamide, carbon disulfide, urea, thiourea, formic and acetic acids were studied. All the synthesized compounds were characterized by spectroscopic means and elemental analysis. Compound 4c exhibited 64% and 72% analgesic activity. Also, compound 4b showed 50% and 65% anti-inflammatory activity. Interestingly these compounds showed one-third of ulcer index of the reference aspirin and diclofenac.
authors.affiliation: National Research Centre, Photochemistry Department (Heterocyclic and Nucleoside Unit), Dokki, Giza, 12622 Cairo, Egypt. profelgazzar@yahoo.com
authors.forename: Abdel-Rahman B A
authors.initials: AR
authors.lastname: El-Gazzar
authors.forename: Hend N
authors.initials: HN
authors.lastname: Hafez
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D008297:Male; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar
chemical_list: C542854:7-amino-6-cyano-5-(4-(1-piperidinyl)-phenyl)-2-thioxopyrido (2,3- d)pyrimidin-4(1H)-one; D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; C115711:PD 173074; D010880:Piperidines; D011743:Pyrimidines; D011744:Pyrimidinones