Synthesis of substituted benzamides as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 but do not cause gastric damage

…, V Santagada, E Perissutti, B Severino, F Fiorino…

Index: Caliendo, Giuseppe; Santagada, Vincenzo; Perissutti, Elisa; Severino, Beatrice; Fiorino, Ferdinando; Warner, Timothy D; Wallace, John L; Ifa, Demian Rocha; Antunes, Edson; Cirino, Giuseppe; De Nucci, Gilberto European Journal of Medicinal Chemistry, 2001 , vol. 36, # 6 p. 517 - 530

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Citation Number: 18

Abstract

Parsalmide (5-amino-N-butyl-2-(2-propynyloxy) benzamide)(5a), is a non-steroidal anti- inflammatory drug (NSAID), commercialised in Italy until 1985 with the brand name of Synovial®, that has been widely used to treat arthritic patient. In addition, it was shown to spare gastric mucosa. Here we have synthesised a series of novel substituted benzamides, related to Parsalmide, and have evaluated their activity in vitro on COX-1 and COX-2 as ...