Bioisosteric Replacement Leading to Biologically Active [2.2] Paracyclophanes with Altered Binding Profiles for Aminergic G-Protein-Coupled Receptors

…, H Hübner, S Löber, P Gmeiner

Index: Skultety, Marika; Huebner, Harald; Loeber, Stefan; Gmeiner, Peter Journal of Medicinal Chemistry, 2010 , vol. 53, # 19 p. 7219 - 7228

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Citation Number: 10

Abstract

Exploring the chemical diversity space of GPCR ligands, we recently discovered [2.2] paracyclophanes as valuable atypical bioisosteres for secondary affinity and selectivity generating moieties. To find out if such an exchange also works for structural moieties that simulate the endogenous neurotransmitter, π1 or π2 or both systems π1 and π2 of three representative privileged structures of types 1, 2, and 3 were replaced by a [2.2] ...