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

Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and secondary conjugation are important components of the processing of this molecule in vivo. We have synthesized metabolites of efavirenz to confirm their...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-03, Vol.11 (5), p.619-622
Main Authors: Markwalder, Jay A., Christ, David D., Mutlib, Abdul, Cordova, Beverly C., Klabe, Ronald M., Seitz, Steven P.
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Benzoxazines
Biological and medical sciences
Biotransformation
Humans
Medical sciences
Molecular Structure
Oxazines - metabolism
Oxazines - pharmacology
Pharmacology. Drug treatments
Reverse Transcriptase Inhibitors - chemical synthesis
Reverse Transcriptase Inhibitors - chemistry
Reverse Transcriptase Inhibitors - pharmacology
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Summary:Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and secondary conjugation are important components of the processing of this molecule in vivo. We have synthesized metabolites of efavirenz to confirm their structure and to evaluate their activity as antivirals. Efavirenz undergoes species-specific metabolism in vivo. Several primary and secondary metabolites were prepared by total synthesis, and their antiviral activities were determined.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00012-9