Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase
Journal Article
·
· Bioorganic and Medicinal Chemistry Letters
- 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.
- 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
Cited by: 5 works
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