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. 2015 Feb 1;25(3):717-20.
doi: 10.1016/j.bmcl.2014.11.060. Epub 2014 Nov 27.

Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors

B Narasimhulu Naidu  1 , Margaret E Sorenson  2 , Manoj Patel  2 , Yasutsugu Ueda  2 , Jacques Banville  2 , Francis Beaulieu  2 , Sagarika Bollini  3 , Ira B Dicker  3 , Helen Higley  3 , Zeyu Lin  3 , Lori Pajor  4 , Dawn D Parker  4 , Brian J Terry  3 , Ming Zheng  4 , Alain Martel  2 , Nicholas A Meanwell  2 , Mark Krystal  3 , Michael A Walker  2
Affiliations

Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors

B Narasimhulu Naidu et al. Bioorg Med Chem Lett. .

Abstract

Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is a validated target for drug discovery. Herein, we report the synthesis, antiviral activity and pharmacokinetic profiles of several C2-carbon-linked heterocyclic pyrimidinone-4-carboxamides that inhibit the strand transfer step of the integration process.

Keywords: HIV-1; Inhibitor; Integrase; Pyrimidine-4-carboxamide; Strand transfer.

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