4-Aminopyrimidines as novel HIV-1 inhibitors.

Venkat R Gadhachanda, Baogen Wu, Zhiwei Wang, Kelli L Kuhen, Jeremy Caldwell, Helmut Zondler, Harald Walter, Mark Havenhand, Yun He

Index: Bioorg. Med. Chem. Lett. 17(1) , 260-5, (2007)

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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.