Issue 20, 2013
From the journal:

Chemical Communications

Organocatalytic multicomponent reaction for the acquisition of a selective inhibitor of mPTPB, a virulence factor of tuberculosis†

Rongjun He,a   Li-Fan Zeng,a   Yantao He,a   Li Wu,a   Andrea Michelle Gunawana  and  Zhong-Yin Zhang*a  

* Corresponding authors

a Department of Biochemistry and Molecular Biology, Chemical Genomics Core Facility, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN, USA
E-mail: zyzhang@iupui.edu
Fax: +1-317-274-4686
Tel: +1-317-274-4686

Abstract

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.

Graphical abstract: Organocatalytic multicomponent reaction for the acquisition of a selective inhibitor of mPTPB, a virulence factor of tuberculosis

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Article information

DOI
https://doi.org/10.1039/C3CC38961H
Article type
Communication
Submitted
14 Dec 2012
Accepted
24 Jan 2013
First published
24 Jan 2013

Chem. Commun., 2013,49, 2064-2066

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Organocatalytic multicomponent reaction for the acquisition of a selective inhibitor of mPTPB, a virulence factor of tuberculosis

R. He, L. Zeng, Y. He, L. Wu, A. Michelle Gunawan and Z. Zhang, Chem. Commun., 2013, 49, 2064 DOI: 10.1039/C3CC38961H

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