2024
DOI: 10.1021/acsinfecdis.3c00525
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N-Substituted Bicyclic Carbamoyl Pyridones: Integrase Strand Transfer Inhibitors that Potently Inhibit Drug-Resistant HIV-1 Integrase Mutants

Pankaj S. Mahajan,
Steven J. Smith,
Min Li
et al.

Abstract: HIV-1 integrase (IN) is an important molecular target for the development of anti-AIDS drugs. A recently FDAapproved second-generation integrase strand transfer inhibitor (INSTI) cabotegravir (CAB, 2021) is being marketed for use in longduration antiviral formulations. However, missed doses during extended therapy can potentially result in persistent low levels of CAB that could select for resistant mutant forms of IN, leading to virological failure. We report a series of N-substituted bicyclic carbamoyl pyrid… Show more

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