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ID: ALA1141522
Journal: Bioorg Med Chem Lett
Title: Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.
Authors: Thoma G, Beerli C, Bigaud M, Bruns C, Cooke NG, Streiff MB, Zerwes HG.
Abstract: Introduction of polar groups in a series of potent CCR5 antagonists which are very likely to adversely affect the conduction system in the heart led to the identification of NIBR-1282 which did not show adverse effects when tested in an isolated rabbit heart ex vivo model. Administration of NIBR-1282 in combination with a non-efficacious dose of CsA led to significant prolongation of kidney allograft survival in cynomolgus monkeys.
CiteXplore: 18267361