Arzneimittelforschung 2008; 58(9): 457-463
DOI: 10.1055/s-0031-1296539
Antiemetics · Gastrointestinal Drugs · Urologic Drugs
Editio Cantor Verlag Aulendorf (Germany)

Synthesis, Analgesic and Anti-inflammatory Activities of Some New Fenamate Analogues

Ahmed M Alafeefy
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
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Publikationsdatum:
19. Dezember 2011 (online)

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Abstract

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.