Diversity-oriented synthesis for novel, selective and drug-like inhibitors for a phosphatase from Mycobacterium tuberculosis

Rongjun He, Yunpeng Bai, Zhi Hong Yu, Li Wu, Andrea Michelle Gunawan, Zhong Yin Zhang

Research output: Contribution to journalArticle

5 Scopus citations

Abstract

Mycobacterium protein tyrosine phosphatase B (mPTPB) is a potential drug target of tuberculosis (TB). Using small molecule inhibitors of mPTPB could be a treatment to overcome emerging TB drug resistance. Using a Diversity-Oriented Synthesis (DOS) strategy, we successfully developed a salicylic acid based and drug-like mPTPB inhibitor with an IC50 of 2 μM and >20-fold specificity over many human PTPs, making it an excellent lead molecule for anti-TB drug discovery. In addition, DOS generated bicyclic salicylic acids are also promising starting points for acquiring inhibitors targeting other PTPs. This journal is

Original languageEnglish (US)
Pages (from-to)1496-1499
Number of pages4
JournalMedChemComm
Volume5
Issue number10
DOIs
StatePublished - Oct 1 2014

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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