Synthesis and histamine H 1-receptor antagonist activity of 4-(diphenylmethyl)-1-piperazine derivatives with a terminal heteroaryl or cycloalkyl amide fragment

…, JC Gil-Sánchez, L Alonso-Cires, L Labeaga…

Index: Orjales; Gil-Sanchez; Alonso-Cires; Labeaga; Mosquera; Berisa; Ucelay; Innerarity; Corcostegui European Journal of Medicinal Chemistry, 1996 , vol. 31, # 10 p. 813 - 818

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Citation Number: 3

Abstract

New 4-(diphenylmethyl)-1-piperazine derivatives with a terminal heteroaryl or cycloalkyl amide fragment were synthesized and evaluated for their antihistaminic, anticholinergic and antiallergic activities. Tested compounds were found to be moderate to potent in vitro (guinea-pig ileum) histamine H1-receptor antagonists. Derivatives with a four methylene chain (1e-1h) were as potent in vivo (capillary permeability in rats) as cetirizine; the ...