The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor
BMS-707035 is an HIV-1 integrase strand transfer inhibitor (INSTI) discovered by systematic optimization of N-methylpyrimidinone carboxamides guided by structure-activity relationships (SARs) and the single crystal X-ray structure of compound 10. It was r
Naidu, B. Narasimhulu,Walker, Michael A.,Sorenson, Margaret E.,Ueda, Yasutsugu,Matiskella, John D.,Connolly, Timothy P.,Dicker, Ira B.,Lin, Zeyu,Bollini, Sagarika,Terry, Brian J.,Higley, Helen,Zheng, Ming,Parker, Dawn D.,Wu, Dedong,Adams, Stephen,Krystal, Mark R.,Meanwell, Nicholas A.
Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors
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.
Naidu, B. Narasimhulu,Sorenson, Margaret E.,Patel, Manoj,Ueda, Yasutsugu,Banville, Jacques,Beaulieu, Francis,Bollini, Sagarika,Dicker, Ira B.,Higley, Helen,Lin, Zeyu,Pajor, Lori,Parker, Dawn D.,Terry, Brian J.,Zheng, Ming,Martel, Alain,Meanwell, Nicholas A.,Krystal, Mark,Walker, Michael A.
p. 717 - 720
(2015/01/30)
HIV Integrase Inhibitors
The invention encompasses a series pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pha
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(2009/01/20)
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