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Bioorg Med Chem Lett. 2008 Jan 1;18(1):147-51. Epub 2007 Nov 4.

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

Author information

1
UCB Inflammation Discovery, Granta Park, Great Abington, Cambridge CB21 6GS, United Kingdom. bob.watson@ucb-group.com

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.

PMID:
18032038
DOI:
10.1016/j.bmcl.2007.10.109
[Indexed for MEDLINE]

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