Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir)

The HIV protease inhibitor ABT-378 (Lopinavir) has a 2,6-dimethylphenoxyacetyl group in the P-2' position. Analogues in which this group is replaced with various substituted phenyl or heteroaryl groups were synthesized and the structure-activity relationships explored.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-04, Vol.12 (8), p.1185-1187
Main Authors: SHAM, Hing L, BETEBENNER, David A, XIAOQI CHEN, SALDIVAR, Ayda, VASAVANONDA, Sudthida, KEMPF, Dale J, PLATTNER, Jacob J, NORBECK, Daniel W
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Cell Line
HIV Protease Inhibitors - chemical synthesis
HIV Protease Inhibitors - chemistry
HIV Protease Inhibitors - pharmacology
Humans
Lopinavir
Medical sciences
Pharmacology. Drug treatments
Pyrimidinones - chemical synthesis
Pyrimidinones - chemistry
Pyrimidinones - pharmacology
Structure-Activity Relationship
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Summary:The HIV protease inhibitor ABT-378 (Lopinavir) has a 2,6-dimethylphenoxyacetyl group in the P-2' position. Analogues in which this group is replaced with various substituted phenyl or heteroaryl groups were synthesized and the structure-activity relationships explored.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00134-8