| Literature DB >> 14627401 |
David M Andrews1, Michael C Barnes, Mike D Dowle, S Lucy Hind, Martin R Johnson, Paul S Jones, Gail Mills, Angela Patikis, Tony J Pateman, Tracy J Redfern, J Ed Robinson, Martin J Slater, Naimisha Trivedi.
Abstract
[reaction: see text] In this, the second of two Letters, the optimization of the pyrrolidine-5,5-trans-lactam template (exemplified by 1a) as a mechanism-based inhibitor of hepatitis C NS3/4A protease is described. "Right Box" analysis of cassette dosing screening pharmacokinetic data was used to rapidly categorize the compounds. GW0014 (compound 4d) emerged as the compound displaying an optimal balance of biochemical and replicon potency, along with low i.v. clearance in the dog.Entities:
Mesh：
Substances：
Year: 2003 PMID： 14627401 DOI： 10.1021/ol035827n
Source DB: PubMed Journal: Org Lett ISSN： 1523-7052 Impact factor: 6.005