Journal
CHEMISTRY-AN ASIAN JOURNAL
Volume 2, Issue 9, Pages 1109-1126Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.200700125
Keywords
alkaloids; biology-oriented synthesis (BIOS); enzyme inhibition; phosphatases; solid-phase synthesis
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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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