Document Detail


Organocatalytic multicomponent reaction for the acquisition of a selective inhibitor of mPTPB, a virulence factor of tuberculosis.
MedLine Citation:
PMID:  23380872     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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 IC(50) 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.
Authors:
Rongjun He; Li-Fan Zeng; Yantao He; Li Wu; Andrea Michelle Gunawan; Zhong-Yin Zhang
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Chemical communications (Cambridge, England)     Volume:  49     ISSN:  1364-548X     ISO Abbreviation:  Chem. Commun. (Camb.)     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-12     Completed Date:  2013-08-16     Revised Date:  2014-03-11    
Medline Journal Info:
Nlm Unique ID:  9610838     Medline TA:  Chem Commun (Camb)     Country:  England    
Other Details:
Languages:  eng     Pagination:  2064-6     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Aniline Compounds / chemistry
Antitubercular Agents / chemical synthesis,  chemistry*,  pharmacology
Bacterial Proteins / antagonists & inhibitors*,  metabolism
Catalysis
Enzyme Inhibitors / chemical synthesis,  chemistry*,  pharmacology
Formaldehyde / chemistry
Mycobacterium tuberculosis / drug effects,  metabolism
Protein Tyrosine Phosphatases / antagonists & inhibitors*,  metabolism
Pyrroles / chemistry
Virulence Factors / antagonists & inhibitors,  metabolism
Grant Support
ID/Acronym/Agency:
CA152194/CA/NCI NIH HHS; R01 CA152194/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Aniline Compounds; 0/Antitubercular Agents; 0/Bacterial Proteins; 0/Enzyme Inhibitors; 0/MptpA protein, Mycobacterium tuberculosis; 0/Pyrroles; 0/Virulence Factors; 1HG84L3525/Formaldehyde; EC 3.1.3.48/Protein Tyrosine Phosphatases; SIR7XX2F1K/aniline
Comments/Corrections

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