The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.

B Narasimhulu Naidu,Michael A Walker,Margaret E Sorenson,Yasutsugu Ueda,John D Matiskella,Timothy P Connolly,Ira B Dicker,Zeyu Lin,Sagarika Bollini,Brian J Terry,Helen Higley,Ming Zheng,Dawn D Parker,Dedong Wu,Stephen Adams,Mark R Krystal,Nicholas A Meanwell

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•Synthesis and antiviral activities of series of pyrimidinone carboxamide described.•BMS-707035 is a potent HIV-1 integrase strand transfer inhibitor.•It displayed good preclinical profiles; advanced to clinical trials.•Development halted due to the findings in 12-month dog safety assessment study.

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关键词

HIV-1 integrase,Strand transfer inhibitors,INSTI,Pyrimidinone carboxamides,Antiviral activity,Pharmacokinetics

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