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

Rongjun He, Li Fan Zeng, Yantao He, Li Wu, Andrea Michelle Gunawan, Zhong-Yin Zhang

Research output: Contribution to journalArticle

15 Citations (Scopus)

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 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.

Original languageEnglish
Pages (from-to)2064-2066
Number of pages3
JournalChemical Communications
Volume49
Issue number20
DOIs
StatePublished - Mar 11 2013

Fingerprint

Protein Tyrosine Phosphatases
Phosphatases
Virulence Factors
Proteins
Pyrroles
Aniline
Formaldehyde
Molecules

ASJC Scopus subject areas

  • Metals and Alloys
  • Materials Chemistry
  • Surfaces, Coatings and Films
  • Electronic, Optical and Magnetic Materials
  • Ceramics and Composites
  • Catalysis
  • Chemistry(all)

Cite this

Organocatalytic multicomponent reaction for the acquisition of a selective inhibitor of mPTPB, a virulence factor of tuberculosis. / He, Rongjun; Zeng, Li Fan; He, Yantao; Wu, Li; Michelle Gunawan, Andrea; Zhang, Zhong-Yin.

In: Chemical Communications, Vol. 49, No. 20, 11.03.2013, p. 2064-2066.

Research output: Contribution to journalArticle

He, Rongjun ; Zeng, Li Fan ; He, Yantao ; Wu, Li ; Michelle Gunawan, Andrea ; Zhang, Zhong-Yin. / Organocatalytic multicomponent reaction for the acquisition of a selective inhibitor of mPTPB, a virulence factor of tuberculosis. In: Chemical Communications. 2013 ; Vol. 49, No. 20. pp. 2064-2066.
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