Ontology highlight
ABSTRACT:
SUBMITTER: Bulut H
PROVIDER: S-EPMC7326966 | biostudies-literature | 2020 Jun
REPOSITORIES: biostudies-literature
Scientific reports 20200630 1
HIV-1 protease inhibitors (PIs), such as darunavir (DRV), are the key component of antiretroviral therapy. However, HIV-1 often acquires resistance to PIs. Here, seven novel PIs were synthesized, by introducing single atom changes such as an exchange of a sulfur to an oxygen, scission of a single bond in P2'-cyclopropylaminobenzothiazole (or -oxazole), and/or P1-benzene ring with fluorine scan of mono- or bis-fluorine atoms around DRV's scaffold. X-ray structural analyses of the PIs complexed wi ...[more]