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TYROSINE PHOSPHATASE INHIBITORS AND USES THEREOF TO MODULATE THE ACTIVITY OF ENZYMESp INVOLVED IN THE PATHOLOGY OF MYCOBACTERIUM TUBERCULOSIS
TYROSINE PHOSPHATASE INHIBITORS AND USES THEREOF TO MODULATE THE ACTIVITY OF ENZYMESp INVOLVED IN THE PATHOLOGY OF MYCOBACTERIUM TUBERCULOSIS
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机译:酪氨酸磷酸酶抑制剂及其用于调节参与结核分枝杆菌病理的酶的活性
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摘要
A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.
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