Synthesis, analgesic and anti inflammatory activities of some new fenamate analogues.
A series of fenamate quinazolinyl analogues, viz acids 6a-d, esters 6e-h, carbohydrazides 7a-d, arylidenes 8a-d, oxadiazol-2-ones 13a-d and oxadiazol-2-thiones 14a-d, have been prepared and screened for their analgesic (acetic acid-induced writhing), anti-inflammatory (carrageenan-induced rat paw edema) activities as well as their ulcerogenic effects. All the final compounds except 7a-d and 8a-d showed good dual activities. Compounds 6a, 6b, 6e, 6f, 13a and 14a showed activities comparable to that of mefenamic acid (CAS 61-68-7) in the acetic acid-induced writhing model as well as in the carrageenan-induced rat paw edema test at a dose level of 100 mg/ kg.Compounds 6a and 6b were highly ulcerogenic, while compounds 6e, 6f, 13a and 14a exhibited the lowest ulcerogenic effects.
Alafeefy
Ahmed M
AM
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. aalafeefy@yahoo.com
D019342:Acetic Acid; D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D002627:Chemistry, Physical; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D054361:Fenamates / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D013055:Spectrophotometry, Infrared; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology
D018712:Analgesics, Non-Narcotic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D054361:Fenamates; D007202:Indicators and Reagents; D019342:Acetic Acid