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Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.

Thoma, Gebhard and Beerli, Christian and Bigaud, Marc and Bruns, Christian and Cooke, Nigel Graham and Streiff, Markus and Zerwes, Hans-Guenter (2008) Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo. Bioorganic & Medicinal Chemistry letters, 18 (6). pp. 2000-2005. ISSN 1464-3405

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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Chemokines; Chemokine receptors; CCR5; Cardiac side-effects; hERG
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Date Deposited: 14 Dec 2009 13:51
Last Modified: 31 Jan 2013 01:03
URI: https://oak.novartis.com/id/eprint/911

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