Ontology highlight
ABSTRACT:
SUBMITTER: Samuels ER
PROVIDER: S-EPMC7179874 | biostudies-literature | 2020 Mar
REPOSITORIES: biostudies-literature
Samuels Eric R ER Sevrioukova Irina F IF
Bioorganic & medicinal chemistry 20200131 6
Identification of structural determinants required for potent inhibition of drug-metabolizing cytochrome P450 3A4 (CYP3A4) could help develop safer drugs and more effective pharmacoenhancers. We utilize a rational inhibitor design to decipher structure-activity relationships in analogues of ritonavir, a highly potent CYP3A4 inhibitor marketed as pharmacoenhancer. Analysis of compounds with the R<sub>1</sub> side-group as phenyl or naphthalene and R<sub>2</sub> as indole or naphthalene in differe ...[more]