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

16 Scopus citations

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 (US)
Pages (from-to)2064-2066
Number of pages3
JournalChemical Communications
Volume49
Issue number20
DOIs
StatePublished - Feb 12 2013

ASJC Scopus subject areas

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

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