| Autor: |
Andrews DM; Department of Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, SG1 2NY, Stevenage, UK. david.m.andrews@gsk.com, Chaignot HM, Coomber BA, Dowle MD, Hind SL, Johnson MR, Jones PS, Mills G, Patikis A, Pateman TJ, Robinson JE, Slater MJ, Trivedi N |
| Jazyk: |
angličtina |
| Zdroj: |
European journal of medicinal chemistry [Eur J Med Chem] 2003 Apr; Vol. 38 (4), pp. 339-43. |
| DOI: |
10.1016/s0223-5234(03)00050-3 |
| Abstrakt: |
The pyrrolidine-5,5-trans-lactam template was used to design small, neutral, mechanism-based inhibitors of hepatitis C NS3/4A protease displaying potent activity in the replicon cell-based assay. The activity of this series is not dependent upon its chemical reactivity and molecules have been synthesised which combine enhanced biochemical potency with improved plasma stability. Promising initial pharmacokinetic data indicating the potential for further optimisation of this series into low molecular weight, drug-like inhibitors is presented. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect