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ID: ALA3632514

Journal: Bioorg Med Chem Lett

Title: Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase.

Authors: Wang H, Liu L, Lu Y, Pan P, Hooker JM, Fowler JS, Tonge PJ.

Abstract: PT70 is a diaryl ether inhibitor of InhA, the enoyl-ACP reductase in the Mycobacterium tuberculosis fatty acid biosynthesis pathway. It has a residence time of 24 min on the target, and also shows antibacterial activity in a mouse model of tuberculosis infection. Due to the interest in studying target tissue pharmacokinetics of PT70, we developed a method to radiolabel PT70 with carbon-11 and have studied its pharmacokinetics in mice and baboons using positron emission tomography.

CiteXplore: 26227776

DOI: 10.1016/j.bmcl.2015.07.019