Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives

…, GA Chapman, FC Galvin, LA Jopling, RL Knight…

Index: Watson, Robert J.; Allen, Daniel R.; Birch, Helen L.; Chapman, Gayle A.; Galvin, Frances C.; Jopling, Louise A.; Knight, Roland L.; Meier, Dorica; Oliver, Kathryn; Meissner, Johannes W.G.; Owen, David A.; Thomas, Elizabeth J.; Tremayne, Neil; Williams, Sophie C. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 147 - 151

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Citation Number: 29

Abstract

The optimization of a series of 1-aryl-3-piperidinyl urea derivatives is described in which incorporation of tropenyl and homotropenyl moieties has led to significant improvements in activity and drug-like properties. Replacement of the central piperidine with an exo-tropanyl unit led to the identification of compound 15 which provides a combination of excellent potency against human and murine receptors, drug-like properties and pharmacokinetics, ...