Expanded-spectrum nonnucleoside reverse transcriptase inhibitors inhibit clinically relevant mutant variants of human immunodeficiency virus type 1

Antimicrobial Agents and Chemotherapy

Volumn 43, Issue 12, 1999, Pages 2893-2897

  Corbett, Jeffrey W ^a   Ko, Soo S ^a   Rodgers, James D ^a   Jeffrey, Susan ^a   Bacheler, Lee T ^a   Klabe, Ronald M ^a   Diamond, Sharon ^a   Lai, Chii Ming ^a   Rabel, Shelley R ^a   Saye, Jo Anne ^a   Adams, Stephen P ^a   Trainor, George L ^a   Anderson, Paul S ^a   Erickson Viitanen, Susan K ^a  

^a DUPONT COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (2 CYCLOPROPYLVINYL) 5,6 DIFLUORO 3,4 DIHYDRO 4 TRIFLUOROMETHYL 2(1H) QUINAZOLINONE; 4 CYCLOPROPYLETHYNYL 5,6 DIFLUORO 3,4 DIHYDRO 4 TRIFLUOROMETHYL 2(1H) QUINAZOLINONE; 4(3H) QUINAZOLINONE DERIVATIVE; 6 CHLORO 4 (2 CYCLOPROPYLVINYL) 3,4 DIHYDRO 4 TRIFLUOROMETHYL 2(1H) QUINAZOLINONE; 6 CHLORO 4 CYCLOPROPYLETHYNYL 3,4 DIHYDRO 4 TRIFLUOROMETHYL 2(1H) QUINAZOLINONE; EFAVIRENZ; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL EXPERIMENT; ARTICLE; CHIMPANZEE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG IDENTIFICATION; DRUG POTENCY; DRUG PROTEIN BINDING; HUMAN IMMUNODEFICIENCY VIRUS 1; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RHESUS MONKEY; VIRUS INHIBITION; VIRUS MUTANT;

EID: 0032786364     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/aac.43.12.2893     Document Type: Article

References (14)

1. Bacheler, L., O. Weislow, S. Snyder, G. Hanna, R. D'Aquila, and the SUSTIVA Resistance Study Team. 1948. Abstract presented at the 12th World AIDS Conference.
2. Bacheler, L. T. 1999. Resistance to non-nucleoside inhibitors of HIV-1. Drug Resist. Updates 2:56-67.
3. Bacheler, L. T., M. Paul, M. J. Otto, P. K. Jadhav, B. A. Stone, and J. A. Miller. 1994. An assay for HIV RNA in infected cell lysates, and its use for rapid evaluation of antiviral efficacy. Antivir. Chem. Chemother. 5:111-121.
4. Corbett, J. W., S. S. Ko, S. K. Erickson-Viitanen, L. T. Bacheler, S. Jeffrey, B. C. Cordova, R. M. Klabe, S. Diamond, J. D. Rodgers, G. L. Trainor, and P. S. Anderson. 1998. Data on DPC 961 and DPC 963 presented in part at the 4th International Congress on Drug Therapy in HIV Infection.
5. Esnouf, R., J. Ran, C. Ross, Y. Jones, D. Stammers, and D. Stuart. 1995. Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors. Nat. Struct. Biol. 2:303-308.
6. Havlir, D. V., S. Eastmen, A. Garnst, and D. D. Richman. 1996. Kinetics of replication and estimated prevalence in untreated patients. J. Virol. 70:7894-7899.
7. Hirsch, M. S. 1998. Resistance to antiretroviral drugs - an emerging problem. AIDS 12:6-7.
8. Jadhav, P. K., P. Ala, F. J. Woerner, C.-H. Chang, S. S. Garber, E. D. Anton, and L. T. Bacheler. 1997. Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild types and protease inhibitor resistant mutants of HIV. J. Med. Chem. 40:181-190.
9. Kleim, J. P., I. Winkler, M. A. Rosner, R. Kirsch, H. Rubsamen-Waigmann, A. Paessens, and G. Riess. 1997. In vitro selection for different mutational patterns in the HIV-1 reverse transcriptase using high and low selective pressure of the nonnucleoside reverse transcriptase inhibitor HBY 097. Virology 231:112-118.
10. Morales-Ramirez, J., K. Tashima, D. Hardy, P. Johnson, M. Nelson, S. Staszewski, D. Labriola, N. Ruiz, and the Study 006 Team. 1998. A phase II, multi-center randomized, open label study to compare the antiretroviral activity and tolerability of efavirenz (EFV) + indinavir (IDV), versus EFV + zidovudine (ZDV) + lamirudine (3TC), versus IDV + 3TC at > 36 weeks [DMP 266-006], abstr. I-103, p. 394. In Program and abstracts of the 38th Interscience Conference on Antimicrobial Agents and Chemotherapy. American Society for Microbiology, Washington, D.C.
11. Patel, M., S. S. Ko, R. J. McHugh, J. A. Markwalder, A. S. Srivastava, B. C. Cordova, R. M. Klabe, S. K. Erickson-Viitanen, G. L. Trainor, and S. P. Seitz. Synthesis and evaluation of analogs of efavirenz (SUSTIVA™) as HIV-1 reverse transcriptase inhibitors. Bioorg. Med. Chem. Lett., in press.
12. Smallheer, J. M., M. J. Otto, C. A. Amarl-Ly, R. A. Earl, M. J. Myers, P. Pennev, D. C. Montefiori, and M. A. Wuonola. 1993. Synthesis and anti-HIV activity of a series of 2-indolinones and related analogs. Antivir. Chem. Chemother. 4:27-39.
13. Tucker, T. J., T. A. Lyle, C. M. Wiscount, S. F. Britcher, S. D. Young, W. M. Sanders, W. C. Lumma, M. E. Goldman, J. A. O'Brien, R. G. Ball, C. F. Homnick, W. A. Schleif, E. A. Emini, J. R. Huff, and P. S. Anderson. 1994. Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. J. Med. Chem. 37:2437-2444.
14. Young, S. D., S. F. Britcher, L. O. Tran, L. S. Payne, W. C. Lumma, T. A. Lyle, J. R. Huff, P. S. Anderson, D. B. Olsen, S. S. Carrol, D. J. Pettibone, J. A. O'Brien, R. G. Ball, S. K. Balani, J. H. Lin, I. Chen, W. A. Schleif, V. V. Sardana, W. J. Long, V. W. Byrnes, and E. A. Emini. 1995. L-743,726 (DMP266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob. Agents Chemother. 39:2602-2605.