Novel S1P1 Receptor Agonists-Part 2: From Bicyclo [3.1. 0] hexane-Fused Thiophenes to Isobutyl Substituted Thiophenes

…, R de Kanter, P Hess, C Kohl, D Lehmann…

Index: Bolli, Martin H.; Velker, Joerg; Mueller, Claus; Mathys, Boris; Birker, Magdalena; Bravo, Roberto; Bur, Daniel; De Kanter, Ruben; Hess, Patrick; Kohl, Christopher; Lehmann, David; Meyer, Solange; Nayler, Oliver; Rey, Markus; Scherz, Michael; Steiner, Beat Journal of Medicinal Chemistry, 2014 , vol. 57, # 1 p. 78 - 97

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Citation Number: 8

Abstract

Previously, we reported on the discovery of a novel series of bicyclo [3.1. 0] hexane fused thiophene derivatives that serve as potent and selective S1P1 receptor agonists. Here, we discuss our efforts to simplify the bicyclohexane fused thiophene head. In a first step the bicyclohexane moiety could be replaced by a simpler, less rigid cyclohexane ring without compromising the S1P receptor affinity profile of these novel compounds. In a second step ...