2. Academic Validation
  3. Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)

Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)

  • J Med Chem. 2008 Feb 28;51(4):875-96. doi: 10.1021/jm701284j.
Jean-François Bonfanti 1,  Christophe Meyer,  Frédéric Doublet,  Jérôme Fortin,  Philippe Muller,  Laurence Queguiner,  Tom Gevers,  Peggy Janssens,  Heidi Szel,  Rudy Willebrords,  Philip Timmerman,  Koen Wuyts,  Pieter van Remoortere,  Frans Janssens,  Piet Wigerinck,  Koen Andries
Affiliations

Affiliation

  • 1 Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research and Development, Campus de Maigremont, BP 615, F-27106 Val de Reuil, France. jbonfant@prdfr.jnj.com
PMID: 18254606 DOI: 10.1021/jm701284j
Abstract

A preceding paper (Bonfanti et al. J. Med Chem. 2007, 50, 4572-4584) reported the optimization of the pharmacokinetic profile of substituted benzimidazoles by reducing their tissue retention. However, the modifications that were necessary to achieve this goal also led to a significant drop in anti-RSV activity. This paper describes a molecular modeling study followed by a lead optimization program that led to the recovery of the initial potent Antiviral activity and the selection of TMC353121 as a clinical candidate.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-11097
    ≥98.0%, RSV抑制剂
    RSV
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