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Spirodiketopiperazine-based CCR5 antagonist: Discovery of an antiretroviral drug candidate

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
21
Issue
4
Identifiers
DOI: 10.1016/j.bmcl.2010.12.109
Keywords
  • Ccr5
  • Chemokine
  • Anti-Hiv
Disciplines
  • Pharmacology

Abstract

Abstract 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.

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