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Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir)
Authors:Sham Hing L  Betebenner David A  Chen Xiaoqi  Saldivar Ayda  Vasavanonda Sudthida  Kempf Dale J  Plattner Jacob J  Norbeck Daniel W
Institution:Pharmaceutical Discovery, D47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. hing.l.sham@abbott.com
Abstract: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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