Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres

Journal of Medicinal Chemistry

Volumn 45, Issue 15, 2002, Pages 3321-3324

  Rocheblave, Luc ^a,b   Bihel, Frédéric ^a,b   De Michelis, Céline ^a,b   Priem, Ghislaine ^a,b   Courcambeek, Jérôme ^a,b   Bonnet, Brice ^a   Chermann, Jean Claude ^b   Kraus, Jean Louis ^a,b  

^a AIX MARSEILLE UNIVERSITY   (France)

^b INSERM   (France)

Author keywords

[No Author keywords available]

Indexed keywords

AMPRENAVIR; AMPRENAVIR DERIVATIVE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; PROTEINASE; PROTEINASE INHIBITOR; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ARTICLE; CELL CULTURE; CHEMICAL MODIFICATION; CONTROLLED STUDY; DIASTEREOISOMER; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INFECTION PREVENTION; NONHUMAN; PROTEINASE INHIBITION;

ANTI-HIV AGENTS; CARBAMATES; CELL LINE; HIV PROTEASE; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; VIRUS REPLICATION;

EID: 0037130225     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0208323     Document Type: Article

References (26)

1. A structural model for the retroviral proteases
2. Nucleotide sequence of SRV-1, a type D simian acquired immune deficiency syndrome
3. Complete nucleotide sequence of the AIDS Virus, HTLV III
4. Nucleoside sequence of the AidsVirus, LAV
5. Nucleic acid structure and expression of the human AIDS/lymphadonopathy retrovirus
6. Active HIV-1 protease is required for viral infectivity
7. HTLV III GAG protein is processed in yeast-cells by the virus pol-protease
8. Identification of MK-944a: A second clinical candidate from the hydroxy-laminepentanamide isostere series of HIV protease inhibitors
9. HIV protease inhibitors
10. Human immunodeficiency virus type-1 protease inhibitors: Therapeutic successes and failures, suppression and resistance
11. Treatment with amprenavir alone or amprenavir with zidovudine and lamivudine in adults with human immunodeficiency virus infection
12. Recent development in HIV protease therapy
13. Changes in drug sensitivity of human immunodeficiency virus type I during therapy with azidothymidine, dideoxycytidine, and dideoxyinosine: An In Vitro Comparative Study
14. Mechanisms of nucleoside analog, antiviral activity and resistance during HIV reverse transcription
15. Antiviral therapy for HIV infections
16. Bioisosterism: A rational appoach in drug design
17. Diastereoselective epoxidation of dipeptides olefins
18. (Hydroxyethyl) Sulfonamide HIV-1 protease inhibitors: Identification of the 2-methylbenzoyl moiety at P-2
19. Activated dimethyl sulfoxyde: Useful reagents for synthesis
20. N,N′-disuccinimidyl carbonate: A useful reagent for alkoxycarbonylation of amines
21. Nitroxyl-mediated electooxidation of alcohols to aldehydes and ketones
22. C-alkylation of peptides through polylithiated and LiCL-solvated derivatives containing sarcosine Li-enolate units
23. Synthesis and anti-HIV activity of α-thiophenoxy-hydroxyethylamide derivative
24. Detection and titration of neutralizing antibodies to HIV using an inhibition of the cytopathic effect of the virus on MT4 cells
25. Productive infection of CD4+ cells by selected HIV strains is not inhibited by anti-CD4 monoclonal antibodies
26. Rapid, sensitive and efficient HPLC assays for HIV-1 proteinase