HCV NS5A replication complex inhibitors. Part 5: discovery of potent and pan-genotypic glycinamide cap derivatives.
| Autor: | Belema M; Department of Medicinal Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. makonen.belema@bms.com, Nguyen VN, St Laurent DR, Lopez OD, Qiu Y, Good AC, Nower PT, Valera L, O'Boyle DR 2nd, Sun JH, Liu M, Fridell RA, Lemm JA, Gao M, Knipe JO, Meanwell NA, Snyder LB |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Aug 01; Vol. 23 (15), pp. 4428-35. Date of Electronic Publication: 2013 May 23. |
| DOI: | 10.1016/j.bmcl.2013.05.040 |
| Abstrakt: | The isoquinolinamide series of HCV NS5A inhibitors exemplified by compounds 2b and 2c provided the first dual genotype-1a/1b (GT-1a/1b) inhibitor class that demonstrated a significant improvement in potency toward GT-1a replicons compared to that of the initial program lead, stilbene 2a. Structure-activity relationship (SAR) studies that uncovered an alternate phenylglycine-based cap series that exhibit further improvements in virology profile, along with some insights into the pharmacophoric elements associated with the GT-1a potency, are described. (Copyright © 2013 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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