2. Academic Validation
  3. Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors

Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors

  • Bioorg Med Chem Lett. 2001 Oct 22;11(20):2683-6. doi: 10.1016/s0960-894x(01)00542-x.
S E Webber 1,  J T Marakovits,  P S Dragovich,  T J Prins,  R Zhou,  S A Fuhrman,  A K Patick,  D A Matthews,  C A Lee,  B Srinivasan,  T Moran,  C E Ford,  M A Brothers,  J E Harr,  J W Meador 3rd,  R A Ferre,  S T Worland
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, La Jolla, 3565 General Atomics Court, San Diego, CA 92121, USA. swebber@anadyspharma.com
PMID: 11591501 DOI: 10.1016/s0960-894x(01)00542-x
Abstract

Novel tripeptidyl C-terminal Michael acceptors with an ester replacement of the P(2)-P(3) amide bond were investigated as irreversible inhibitors of the human rhinovirus (HRV) 3C protease (3CP). When screened against HRV serotype-14 the best compound was shown to have very good 3CP inhibition (k(obs)/[I]=270,000M(-1)s(-1)) and potent in vitro Antiviral activity (EC(50)=7.0nM).

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