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. 2014 Aug 18:83:609-16.
doi: 10.1016/j.ejmech.2014.06.061. Epub 2014 Jun 28.

Pyridopyrimidinone inhibitors of HIV-1 RNase H

Emile J Velthuisen  1 , Brian A Johns  2 , Peter Gerondelis  2 , Yan Chen  2 , Ming Li  2 , Ke Mou  2 , Wenwen Zhang  2 , John W Seal  2 , Kendra E Hightower  2 , Sonia R Miranda  2 , Kevin Brown  2 , Lisa Leesnitzer  2
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Pyridopyrimidinone inhibitors of HIV-1 RNase H

Emile J Velthuisen et al. Eur J Med Chem. .

Abstract

Using a structure based pharmacophore design, a weak inhibitor of RNase H, identified from a small library of two metal binding HIV-1 integrase inhibitors, was optimized for potency and physicochemical properties. This manuscript describes the SAR and in vivo DMPK for the pyridopyrimidinone class of inhibitors.

Keywords: AIDS; Endonuclease; HIV; Integrase; Reverse transcriptase; Two-metal binder.

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