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2004
Pyrazine derivatives
R 0550
P1' Oxadiazole Protease Inhibitors with Excellent Activity Against Native and
Inhibitor-Resistant HIV-1. — HIV protease inhibitors containing oxadiaz51- 136 Protease
oles at the P1' position are synthesized by a novel approach involving the stereospecific
introduction of a P1' carboxylic acid, enabling the installation of a variety of heterocycles at that position. The key step in the synthesis of representative oxadiazole (XIII)
consists of the diastereoselective allylation of protected hydroxybutyramide (IV). Conversion of carboxylic acid (VII) to hydrazide (VIII) under peptide coupling conditions,
heterocycle formation under nonacidic conditions, and assembling the final product by
established procedures complete the synthetic approach. All of the P1' oxadiazoles are
picomolar inhibitors of native HIV-1 protease, and most of the oxadiazoles maintain
excellent antiviral activity against a panel of HIV-1 protease inhibitor-resistant strains.
— (KIM*, R. M.; ROUSE, E. A.; CHAPMAN, K. T.; SCHLEIF, W. A.; OLSEN, D.
B.; STAHLHUT, M.; RUTKOWSKI, C. A.; EMINI, E. A.; TATA, J. R.; Bioorg.
Med. Chem. Lett. 14 (2004) 18, 4651-4654; Dep. Basic Chem., Merck Res. Lab.,
Rahway, NJ 07065, USA; Eng.) — H. Hoennerscheid
2004
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