330555-74-3Relevant academic research and scientific papers
Nucleotide competing reverse transcriptase inhibitors: Discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors
James, Clint A.,Deroy, Patrick,Duplessis, Martin,Edwards, Paul J.,Halmos, Teddy,Minville, Joannie,Morency, Louis,Morin, Sébastien,Simoneau, Bruno,Tremblay, Martin,Bethell, Richard,Cordingley, Michael,Duan, Jianmin,Lamorte, Louie,Pelletier, Alex,Rajotte, Daniel,Salois, Patrick,Tremblay, Sonia,Sturino, Claudio F.
supporting information, p. 2781 - 2786 (2013/06/27)
A HTS screen led to the identification of a benzofurano[3,2-d]pyrimidin-2- one core structure which upon further optimization resulted in 1 as a potent HIV-1 nucleotide competing reverse transcriptase inhibitor (NcRTI). Investigation of the SAR at N-1 allowed significant improvements in potency and when combined with the incorporation of heterocycles at C-8 resulted in potent analogues not requiring a basic amine to achieve antiviral activity. Additional modifications at N-1 resulted in 33 which demonstrated excellent antiviral potency and improved physicochemical properties.
INHIBITORS OF HIV REPLICATION
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Page/Page column 46, (2010/11/03)
Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.
