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Department of Biochemistry and Molecular Biology, Chemical Genomics Core Facility, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, USA
; Fax: +1-317-274-4686
; Tel: +1-317-274-4686
Chem. Commun., 2013,49, 2064-2066
14 Dec 2012,
24 Jan 2013
First published online
24 Jan 2013
Mycobacterium protein tyrosine phosphatase B (mPTPB) is essential for the survival and persistence of Mycobacterium in the host. Thus small molecule inhibitors of mPTPB are potential anti-TB agents. We developed an efficient organocatalytic multicomponent reaction (MCR) between pyrrole, formaldehyde and aniline, affording a potent and selective mPTPB inhibitor with an IC50 value of 1.5 μM and >50-fold specificity. Our studies provide a successful example of using organocatalysis as a discovery tool for the acquisition of PTP inhibitors.
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