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SYNTHESIS AND BIOLOGICAL EVALUATION OF INHIBITORS OF BOTULINUM NEUROTOXIN METALLOPROTEASE

  1. Author:
    Wang, C. B.
    Widom, J.
    Petronijevic, F.
    Burnett, J. C.
    Nuss, J. E.
    Bavari, S.
    Gussio, R.
    Wipf, P.

  2. Author Address

    Wang, Chenbo, Widom, Julia, Petronijevic, Filip, Wipf, Peter] Univ Pittsburgh, Dept Chem, Pittsburgh, PA 15260 USA. [Burnett, James C.] NCI, Target Struct Based Drug Discovery Grp, SAIC Frederick Inc, Frederick, MD 21702 USA. [Nuss, Jonathan E.; Bavari, Sina] USA, Med Res Inst Infect Dis, Ft Detrick, MD 21702 USA. [Gussio, Rick] NCI, Informat Technol Branch, Dev Therapeut Program, Frederick, MD 21702 USA.
    1. Year: 2009
  2. Journal: Heterocycles
    1. 79
    2. Pages: 487-520
  4. Type of Article: Article
  1. Abstract:

    Based on the lead therapeutic agent NSC 240898, a new series of heterocyclic inhibitors of the BoNT serotype A metalloprotease has been generated. Highlights of the synthetic sequences include Sonogashira couplings of polysubstituted building blocks and gold-catalyzed indole formations. Preliminary structure-activity relationship studies afford detailed insights into the steric and electrostatic properties of the pharmacophore of this molecular scaffold.

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  2. DOI: 10.3987/com-08-s(d)8
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