Synthesis and structure–activity relationships of γ-carboline derivatives as potent and selective cysLT 1 antagonists

…, D Pérez, L Soca, M Miralpeix, D Vilella, P Anton…

Index: Bonjoch, Josep; Diaba, Faiza; Pages, Lluis; Perez, Daniel; Soca, Lidia; Miralpeix, Montserrat; Vilella, Dolors; Anton, Paquita; Puig, Carles Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4299 - 4302

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Citation Number: 11

Abstract

One of the chemical series we have designed in order to achieve this goal is based on the antiH 1 derivative mebhydroline. 6 Taking into account the pharmacophoric model for cysLT 1 antagonists, 7 we expected that the introduction of a quinoline-type substituent in the benzyl group of mebhydroline and an acid group branching from the piperidine moiety (see Fig. 1) would confer a cysLT 1 antagonistic character to the resulting structure (eg 1, see Fig. 2).