Slater Martin J, Andrews David M, Baker Graham, Bethell Susanne S, Carey Seb, Chaignot Helene, Clarke Berwyn, Coomber Barry, Ellis Malcolm, Good Andrew, Gray Norman, Hardy George, Jones Paul, Mills Gail, Robinson Ed
GlaxoSmithKline Medicines Research Centre, Stevenage, UK.
Bioorg Med Chem Lett. 2002 Dec 2;12(23):3359-62. doi: 10.1016/s0960-894x(02)00789-8.
Using a pyrrolidine-5,5-trans-lactam template, we have designed small, neutral, mechanism-based inhibitors of hepatitis C NS3/4A protease. Compound 11a, with an alpha-ethyl P1 substituent and a Boc-valine substituent at the pyrrolidine nitrogen, has an IC(50)=30 microM.
