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Orally bioavailable competitive CCR5 antagonists.

Thoma, Gebhard and Nuninger, Francois and Schaefer, Marc and Akyel, Kayhan Gabriel and Albert, Rainer and Beerli, Christian and Bruns, Christian and Francotte, Eric and Luyten, Marcel and Mackenzie, Duncan and Oberer, Lukas and Streiff, Markus and Wagner, Beatrix and Walter, Hansrudolf and Weckbecker, Gisbert and Zerwes, Hans-Guenter (2004) Orally bioavailable competitive CCR5 antagonists. Journal of Medicinal Chemistry, 47 (8). pp. 1939-1955. ISSN 0022-2623

Abstract

The chemokine receptor CCR5 plays an important role in inflammatory and autoimmune disorders as well as in transplant rejection by affecting the trafficking of effector T cells and monocytes to diseased tissues. Antagonists of CCR5 are believed to be of potential therapeutic value for the disorders mentioned above and HIV infection. Here we report on the structure-activity relationship of a new series of highly potent and selective competitive CCR5 antagonists. While all compounds tested were inactive on rodent CCR5, this series includes compounds that cross-react with the cynomolgus monkey (cyno) receptor. One of these compounds, i.e., 26n, has good PK properties in cynos, and its overall favorable profile makes it a promising candidate for in vivo profiling in transplantation and other disease models.

Item Type: Article
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Date Deposited: 14 Dec 2009 13:54
Last Modified: 31 Jan 2013 01:07
URI: https://oak.novartis.com/id/eprint/765

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