My NCBISign In

Display Settings:

Format

Send to:

Choose Destination
    J Med Chem. 2008 Feb 28;51(4):875-96. Epub 2008 Feb 7.

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

    Bonfanti JF, Meyer C, Doublet F, Fortin J, Muller P, Queguiner L, Gevers T, Janssens P, Szel H, Willebrords R, Timmerman P, Wuyts K, van Remoortere P, Janssens F, Wigerinck P, Andries K.

    Source

    Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research and Development, Campus de Maigremont, BP 615, F-27106 Val de Reuil, France. jbonfant@prdfr.jnj.com

    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.

    PMID:
    18254606
    [PubMed - indexed for MEDLINE]

    MeSH Terms, Substances

    MeSH Terms

    Substances

    LinkOut - more resources

    Full Text Sources

    Other Literature Sources

      Supplemental Content

      Click here to read

      Related citations

      See reviews... See all...

      Cited by 7 PubMed Central articles

      See all...

      Related information

      • Related Citations
        Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
      • BioAssay
        PubChem BioAssay experiments on the biological activities of small molecules that cite the current articles. The depositors of BioAssay data provide these references.
      • Substance (MeSH Keyword)
        PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
      • Cited in PMC
        Full-text articles in the PubMed Central Database that cite the current articles.

      Recent activity

      Clear Turn Off Turn On

      Your browsing activity is empty.

      Activity recording is turned off.

      Turn recording back on

      See more...
      You are here: NCBI > Literature > PubMed
      Write to the Help Desk