Synthesis and evaluation of analogs of Efavirenz (SUSTIVA(TM)) as HIV-1 reverse transcriptase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 19, 1999, Pages 2805-2810

  Patel, Mona ^a   Ko, Soo S ^a   McHugh Jr , Robert J ^a   Markwalder, Jay A ^a   Srivastava, Anurag S ^a   Cordova, Beverly C ^a   Klabe, Ronald M ^a   Erickson Viitanen, Susan ^a   Trainor, George L ^a   Seitz, Steven P ^a  

^a DUPONT COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOXAZINONE DERIVATIVE; EFAVIRENZ; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ARTICLE; DRUG ACTIVITY; DRUG SYNTHESIS; ENZYME ACTIVITY; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MUTATION;

ANTI-HIV AGENTS; HIV-1; MOLECULAR STRUCTURE; OXAZINES; REVERSE TRANSCRIPTASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 0033523619     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00486-2     Document Type: Article

References (10)

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5. th September, 1998.
6. 19F NMR, CIMS/ESIMS, and HRMS/peak match) and were homogeneous by TLC.
7. 90 according to the protocol described in: Bacheler, L. T.; Paul, M.; Jadhav, P. K.; Otto, M.; Miller, J. Antiviral Chem. Chemother. 1994, 5, 111.
8. 90 according to the protocol described in: Bacheler, L. T.; Paul, M.; Jadhav, P. K.; Otto, M.; Miller, J. Antiviral Chem. Chemother. 1994, 5, 111.
9. 8. The data presented for Efavirenz reflects values determined for a single enantiomer, whereas the data shown for 4a-q are that of racemic mixtures. The biological evaluation of each enantiomer of Efavirenz and other benzoxazinones has determined that only the S enantiomer is active.
10. 9. Markwalder, J. A.; Seitz, S. P.; Christ, D. D.; Mutlib, A. Presented at the 26th National Medicinal Chemistry Symposium, Richmond, VA, June 14-18, 1998; Abstract A-23.