4-Aminopyrimidines as novel HIV-1 inhibitors

  • Bioorg Med Chem Lett. 2007 Jan 1;17(1):260-5. doi: 10.1016/j.bmcl.2006.09.047.
Venkat R Gadhachanda  1 ,  Baogen Wu ,  Zhiwei Wang ,  Kelli L Kuhen ,  Jeremy Caldwell ,  Helmut Zondler ,  Harald Walter ,  Mark Havenhand ,  Yun He
Affiliations
  • 1. Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
PMID: 17035019 DOI: 10.1016/j.bmcl.2006.09.047
Abstract

A series of 4-aminopyrimidines (1) was identified as novel HIV inhibitors of unknown molecular target. Structural modifications were carried out to establish its SAR and identify the linking site for target identification. A number of analogs were found to possess single digit inhibitory activity for HIV replication. Several analogs with various potential linkers, including a biotinated analog, also exhibited excellent potency, and could serve as tools for the identification of novel anti-HIV targets.