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Diversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosis

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


Mycobacterium protein tyrosine phosphatase B (mPTPB) is a potential drug target of Tuberculosis (TB). 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

Topics: Mycobacterium protein tyrosine phosphatase B, Tuberculosis, TB drug resistance
Publisher: Royal Society of Chemistry
Year: 2014
DOI identifier: 10.1039/C4MD00099D
OAI identifier:
Provided by: IUPUIScholarWorks

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