Synthesis and structure-activity relationships of novel histamine H1 antagonists: Indolylpiperidinyl benzoic acid derivatives

…, F Antón, Á Cárdenas, D Vilella, M Aparici…

Index: Fonquerna, Silvia; Miralpeix, Montse; Pages, Lluis; Puig, Carles; Cardus, Arantxa; Anton, Francisca; Cardenas, Alvaro; Vilella, Dolors; Aparici, Monica; Calaf, Elena; Prieto, Jose; Gras, Jordi; Huerta, Josep M.; Warrellow, Graham; Beleta, Jorge; Ryder, Hamish Journal of Medicinal Chemistry, 2004 , vol. 47, # 25 p. 6326 - 6337

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Citation Number: 19

Abstract

A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H1 antagonists. Structure-activity relationship studies were directed toward improving in vivo activity and pharmacokinetic profile of our first lead (1). Substitution of fluorine in position 6 on the indolyl ring led to higher in vivo activity in the inhibition of histamine-induced cutaneous vascular permeability assay but lower selectivity toward ...