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Journal/Book: Chem Asian J
Published: 2007
Pages: 1109–1126
Volume: 2
Issue:
Accession no.: 144
Publisher:
ISBN:

Identification of inhibitors for mycobacterial protein tyrosine phosphatase B (MptpB) by biology-oriented synthesis (BIOS).

Ivan R Corrêa, Andrea Nören-Müller, Horst-Dieter Ambrosi, Sven Jakupovic, Krishna Saxena, Harald Schwalbe, Markus Kaiser, Herbert Waldmann
Abstract:
Protein phosphatases have recently emerged as important targets for research in chemical biology and medicinal chemistry, and new classes of phosphatase inhibitors are in high demand. BIOS (biology-oriented synthesis) employs the criteria of relevance to nature and biological prevalidation for the design and synthesis of compound collections. In an application of the BIOS principle, an efficient solid-phase synthesis of highly substituted indolo[2,3-a]quinolizidines by using a vinylogous Mannich-Michael reaction in combination with phosgene- or acid-mediated ring closure was developed. Screening of this library for phosphatase inhibitors yielded a new inhibitor class for the Mycobacterium tuberculosis phosphatase MptpB.
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Prof. Dr. Harald Schwalbe
Institut für Organische Chemie und Chemische Biologie
Johann Wolfgang Goethe Universität
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