Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues

  • Bioorg Med Chem Lett. 2001 Sep 3;11(17):2235-9. doi: 10.1016/s0960-894x(01)00412-7.
D W Ludovici  1 ,  B L De Corte ,  M J Kukla ,  H Ye ,  C Y Ho ,  M A Lichtenstein ,  R W Kavash ,  K Andries ,  M P de Béthune ,  H Azijn ,  R Pauwels ,  P J Lewi ,  J Heeres ,  L M Koymans ,  M R de Jonge ,  K J Van Aken ,  F F Daeyaert ,  K Das ,  E Arnold ,  P A Janssen
Affiliations
  • 1. Janssen Research Foundation, Welsh and McKean Roads, Spring House, PA 19477, USA.
Abstract

The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside Reverse Transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.

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