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Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships |
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| Authors: | Sham Hing L Betebenner David A Rosenbrook William Herrin Thomas Saldivar Ayda Vasavanonda Sudthida Plattner Jacob J Norbeck Daniel W |
| Institution: | Pharmaceutical Discovery, R4MA 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 six-member cyclic urea in the P-2 position. A series of analogues in which the six-member cyclic urea is replaced by various heterocycles was synthesized and the structure-activity relationships explored. |
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