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 structure and to evaluate their activity as antivirals.
DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. jay.a.markwalder@dupontpharma.com
J A
JA
Markwalder
D D
DD
Christ
A
A
Mutlib
B C
BC
Cordova
R M
RM
Klabe
S P
SP
Seitz
D000480:Alkynes; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D048588:Benzoxazines; D001711:Biotransformation; D003521:Cyclopropanes; D006801:Humans; D015394:Molecular Structure; D010078:Oxazines / Q000378:metabolism* / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000480:Alkynes; D000998:Antiviral Agents; D048588:Benzoxazines; D003521:Cyclopropanes; D010078:Oxazines; D018894:Reverse Transcriptase Inhibitors; C098320:efavirenz