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

Artigo Revisado por pares

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

2008; Elsevier BV; Volume: 18; Issue: 6 Linguagem: Inglês

10.1016/j.bmcl.2008.01.108

ISSN

1464-3405

Autores

Gebhard Thoma, Christian Beerli, Marc Bigaud, Christian Bruns, Nigel G. Cooke, Markus Streiff, Hans‐Günter Zerwes,

Tópico(s)

Neuropeptides and Animal Physiology

Resumo

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.

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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