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Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles |
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| Authors: | Rémy C Lemoine Ann C Petersen Lina Setti Jutta Wanner Andreas Jekle Gabrielle Heilek André deRosier Changhua Ji Pamela Berry David Rotstein |
| Institution: | 1. Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA;2. Department of Viral Diseases, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA;3. DMPK, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 9430, USA |
| Abstract: | Replacement of a secondary amide with an N-acyl or N-sulfonyl gem-disubstituted azacyle in a series of CCR5 antagonists led to the identification of compounds with excellent in vitro HIV antiviral activity and increased intrinsic membrane permeability. |
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