title: Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease.
abstract: A potent and novel class of product-like inhibitors of the HCV NS3 protease was discovered by employing a phosphinic acid as a carboxylate isostere. The replicon activity and pharmacokinetic profile of this series of compounds was optimized by exploring the substitution of the phosphinic acid, as well as conformationally constraining these compounds through macrocyclization. The syntheses and preliminary biological evaluation of these phosphinic acids is described.
authors: Gilead Sciences, Inc., 333 Lakeside Dr., Foster City, CA 94404, USA. Michael.Clarke@gilead.com
authors: Michael O
authors: MO
authors: Clarke
authors: Xiaowu
authors: X
authors: Chen
authors: Aesop
authors: A
authors: Cho
authors: William E
authors: WE
authors: Delaney
authors: Edward
authors: E
authors: Doerffler
authors: Maria
authors: M
authors: Fardis
authors: Mingzhe
authors: M
authors: Ji
authors: Michael
authors: M
authors: Mertzman
authors: Rowchanak
authors: R
authors: Pakdaman
authors: Hyun-Jun
authors: HJ
authors: Pyun
authors: Tanisha
authors: T
authors: Rowe
authors: Cheng Y
authors: CY
authors: Yang
authors: X Christopher
authors: XC
authors: Sheng
authors: Choung U
authors: CU
authors: Kim