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 Citations (Scopus)

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

Fingerprint

Protein Tyrosine Phosphatases
Mycobacterium
Mycobacterium tuberculosis
Phosphoric Monoester Hydrolases
Tuberculosis
Pharmaceutical Preparations
Molecules
Salicylic Acid
Salicylates
Drug Discovery
Drug Resistance
Inhibitory Concentration 50

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

Cite this

Diversity-oriented synthesis for novel, selective and drug-like inhibitors for a phosphatase from Mycobacterium tuberculosis. / He, Rongjun; Bai, Yunpeng; Yu, Zhi Hong; Wu, Li; Gunawan, Andrea Michelle; Zhang, Zhong-Yin.

In: MedChemComm, Vol. 5, No. 10, 01.10.2014, p. 1496-1499.

Research output: Contribution to journalArticle

He, Rongjun ; Bai, Yunpeng ; Yu, Zhi Hong ; Wu, Li ; Gunawan, Andrea Michelle ; Zhang, Zhong-Yin. / Diversity-oriented synthesis for novel, selective and drug-like inhibitors for a phosphatase from Mycobacterium tuberculosis. In: MedChemComm. 2014 ; Vol. 5, No. 10. pp. 1496-1499.
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