From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 2, 2007, Pages 350-353

  Petrocchi, Alessia ^a   Koch, Uwe ^a   Matassa, Victor G ^c   Pacini, Barbara ^a   Stillmock, Kara A ^b   Summa, Vincenzo ^a  

^a IRBM   (Italy)

^b MRL   (United States)

^c NONE

Author keywords

HIV integrase inhibitors

Indexed keywords

AMIDE; CARBOXYLIC ACID DERIVATIVE; INTEGRASE INHIBITOR;

ARTICLE; DRUG IDENTIFICATION; ENZYMATIC ASSAY; HUMAN IMMUNODEFICIENCY VIRUS 1; STRUCTURE ACTIVITY RELATION;

AMIDES; HEPACIVIRUS; HIV INTEGRASE INHIBITORS; INDICATORS AND REAGENTS; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; VIRAL NONSTRUCTURAL PROTEINS;

HEPATITIS C VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 33846199468     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.10.054     Document Type: Article

References (12)

1. Pommier Y., Johnson A.A., and Marchand C. Nat. Rev. 4 (2005) 236
2. Fesen M.R., Kohn K.W., Leteurtre F., and Pommier Y. Proc. Natl. Acad. Sci. U.S.A. 90 (1993) 2399
3. Pommier Y., Johnson A.A., and Marchand C. Curr. Top. Med. Chem. (2004) 1059
4. Zhuang L., Wai J.S., Embrey M.W., Fisher T.S., Egbertson M.S., Payne L.P., Guare Jr. J.P., Vacca J.P., Hazuda D.J., Felock P.J., Wolfe A.L., Stillmock K.A., Witmer M.V., Moyer G., Schleif W.A., Gabryelski L.J., Leonard Y.M., Lynch Jr. J.J., Michelson S.R., and Young S.D. J. Med. Chem. 46 (2003) 453
5. Hazuda D.J., Anthony N.J., Gomez R.P., Jolly S.M., Wai J.S., Zhuang L., Fisher T.E., Embrey M., Guare Jr. J.P., Egbertson M.S., Vacca J.P., Huff J.R., Felock P.J., Witmer M.V., Stillmock K.A., Danovich R., Grobler J., Miller M.D., Espeseth A.S., Jin L., Chen I.-W., Lin J.H., Kassahun K., Ellis J.D., Wong B.K., Xu W., Pearson P.G., Schleif W.A., Cortese R., Emini E., Summa V., Holloway M.K., and Young S.D. Proc. Natl. Acad. Sci. 101 (2004) 11233
6. Summa V., Petrocchi A., Pace P., Matassa V., De Francesco R., Altamura S., Tomei L., Koch U., and Neuner P. J. Med. Chem. 47 (2004) 14
7. Pace P., Nizi E., Pacini B., Pesci S., Matassa V., De Francesco R., Altamura S., and Summa V. Bioorg. Med. Chem. Lett. 14 (2004) 3257
8. Summa V., Petrocchi A., Matassa V., Taliani M., Laufer R., De Francesco R., Altamura S., and Pace P. J. Med. Chem. 47 (2004) 5336
9. Stansfield I., Avolio S., Colarusso S., Gennari N., Narjes F., Pacini B., Ponzi S., and Harper S. Bioorg. Med. Chem. Lett. 14 (2004) 5085
10. Culbertson T.P. J. Heterocycl. Chem. 16 (1979) 1423
11. log P values were calculated using the ACD PhysChem program suite, version 8.00.
12. Summa, V., et al. J. Med. Chem., in press.