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Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 1999 Oct 04; Vol. 9 (19), pp. 2805-10. - Publication Year :
- 1999
-
Abstract
- Efavirenz (SUSTIVA) is a potent non-nucleoside reverse transcriptase inhibitor. Due to the observation of breakthrough mutations of the reverse transcriptase enzyme during Efavirenz therapy, we sought to develop an optimized second generation series. To that end, SAR of the substituents on the aromatic ring was undertaken and the results are summarized here. The 5,6-difluoro (4f) and the 6-methoxy (4m) substituted benzoxazinones were determined to be equipotent, and as a result such substitution patterns will be incorporated in second generation scaffolds.
- Subjects :
- Alkynes
Anti-HIV Agents pharmacology
Benzoxazines
Cyclopropanes
Molecular Structure
Oxazines pharmacology
Reverse Transcriptase Inhibitors pharmacology
Structure-Activity Relationship
Anti-HIV Agents chemical synthesis
HIV-1
Oxazines chemical synthesis
Oxazines chemistry
Reverse Transcriptase Inhibitors chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 9
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 10522695
- Full Text :
- https://doi.org/10.1016/s0960-894x(99)00486-2