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

Wang, Hui; Liu, Li; Lu, Yang; Pan, Pan; Hooker, Jacob M.; Fowler, Joanna S.; Tonge, Peter J.

doi:10.1016/j.bmcl.2015.07.019

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

Journal Article · Tue Jul 14 00:00:00 EDT 2015 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2015.07.019· OSTI ID:1239783

Wang, Hui ^[1]; Liu, Li ^[1]; Lu, Yang ^[1]; Pan, Pan ^[1]; Hooker, Jacob M. ^[2]; Fowler, Joanna S. ^[2]; Tonge, Peter J. ^[1]

Stony Brook Univ., NY (United States)
Brookhaven National Lab. (BNL), Upton, NY (United States)

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.

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Research Organization:: Brookhaven National Lab. (BNL), Upton, NY (United States)

Sponsoring Organization:: National Institute of Health

Grant/Contract Number:: SC00112704

OSTI ID:: 1239783

Report Number(s):: BNL-111671-2015-JA; R&D Project: MO-085; KP1503010

Journal Information:: Bioorganic and Medicinal Chemistry Letters, Vol. 25, Issue 21; ISSN 0960-894X

Country of Publication:: United States

Language:: English

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Cited by: 5 works

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

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