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Bioorg Med Chem Lett. 2011 Feb 15;21(4):1141-5. doi: 10.1016/j.bmcl.2010.12.109. Epub 2010 Dec 28.

Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.

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  • 1Medicinal Chemistry Research Laboratory, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan.


Following the discovery that hydroxylated derivative 3 (Fig. 1) was one of the oxidative metabolites of the original lead 1, it was found that hydroxylated compound 4 possesses higher in vitro anti-HIV potency than the corresponding non-hydroxylated compound 2. Structural hybridation of 4 with the orally available analog 5 resulted in another orally-available spirodiketopiperazine CCR5 antagonist 6a that possesses more favorable pharmaceutical profile for use as a drug candidate.

Copyright © 2010 Elsevier Ltd. All rights reserved.

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