Novel S1P1 receptor agonists− part 3: from thiophenes to pyridines

…, R de Kanter, C Kohl, J Grimont, P Hess…

文献索引：Bolli, Martin H.; Abele, Stefan; Birker, Magdalena; Bravo, Roberto; Bur, Daniel; De Kanter, Ruben; Kohl, Christopher; Grimont, Julien; Hess, Patrick; Lescop, Cyrille; Mathys, Boris; Mueller, Claus; Nayler, Oliver; Rey, Markus; Scherz, Michael; Schmidt, Gunther; Seifert, Juergen; Steiner, Beat; Velker, Joerg; Weller, Thomas Journal of Medicinal Chemistry, 2014 , vol. 57, # 1 p. 110 - 130

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被引用次数: 13

摘要

In preceding communications we summarized our medicinal chemistry efforts leading to the identification of potent, selective, and orally active S1P1 agonists such as the thiophene derivative 1. As a continuation of these efforts, we replaced the thiophene in 1 by a 2-, 3-, or 4-pyridine and obtained less lipophilic, potent, and selective S1P1 agonists (eg, 2) efficiently reducing blood lymphocyte count in the rat. Structural features influencing the compounds' ...