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

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.

DOI: 10.1016/j.bmcl.2015.07.019

Cite this paper

@article{Wang2015RadiolabellingAP, title={Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase.}, author={Hui Wang and Li Liu and Yang Lu and P . K . Pan and Jacob M. Hooker and Joanna S. Fowler and Peter J. Tonge}, journal={Bioorganic & medicinal chemistry letters}, year={2015}, volume={25 21}, pages={4782-6} }