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ID: ALA1140788

Journal: Bioorg Med Chem Lett

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

Authors: Watson RJ, Allen DR, Birch HL, Chapman GA, Galvin FC, Jopling LA, Knight RL, Meier D, Oliver K, Meissner JW, Owen DA, Thomas EJ, Tremayne N, Williams SC.

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, thus providing a valuable tool for the evaluation of CXCR3 antagonists in models of human disease.

CiteXplore: 18032038

DOI: 10.1016/j.bmcl.2007.10.109