A Triazinone Derivative Inhibits HIV-1 Replication by Interfering with Reverse Transcriptase Activity.

ABSTRACT: A novel HIV-1 inhibitor, 6-(tert-butyl)-4-phenyl-4-(trifluoromethyl)-1H,3H-1,3,5-triazin-2-one (compound 1), was identified from a compound library screened for the ability to inhibit HIV-1 replication. EC₅₀ values of compound 1 were found to range from 107.9 to 145.4 nm against primary HIV-1 clinical isolates. In in vitro assays, HIV-1 reverse transcriptase (RT) activity was inhibited by compound 1 with an EC₅₀ of 4.3 μm. An assay for resistance to compound 1 selected a variant of HIV-1 with a RT mutation (RT^L100I ); this frequently identified mutation confers mild resistance to non-nucleoside RT inhibitors (NNRTIs). A recombinant HIV-1 bearing RT^L100I exhibited a 41-fold greater resistance to compound 1 than the wild-type virus. Compound 1 was

SUBMITTER: Urano E 

PROVIDER: S-EPMC7754980 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature