Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz

Authors
Markwalder, JA Mutlib, DDCA Cordova, BC Klabe, RM Seitz, SP
Citation
Ja. Markwalder et al., Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz, BIOORG MED, 11(5), 2001, pp. 619-622
Citations number
10
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
5
Year of publication
2001
Pages
619 - 622
Database
ISI
SICI code
0960-894X(20010312)11:5<619:SABAOP>2.0.ZU;2-4
Abstract
Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and se condary conjugation are important components of the processing of this mole cule in vivo. We have synthesized metabolites of efavirenz to confirm their structure and to evaluate their activity as antivirals. (C) 2001 DuPont Ph armaceuticals Company. Published by Elsevier Science Ltd. All rights reserv ed.