Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties

…, JM Caldero, J Roca, E Garcia, G Romero…

Index: Monge; Del Carmen Pena; Palop; Caldero; Roca; Garcia; Romero; Del Rio; Lasheras Journal of Medicinal Chemistry, 1994 , vol. 37, # 9 p. 1320 - 1325

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Citation Number: 26

Abstract

New 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives were prepared and tested as 5-HT3 receptor antagonists. Some of the new compounds antagonized the effect of 5-HT at the longitudinal muscle myenteric plexus (LMMP) preparation of the guinea pig ileum, and two benzothiazole derivatives, compounds 20 and 2f, were more potent than ondansetron in this regard. However, these two compounds were much weaker than the ...