Peer-reviewed veterinary case report
Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2015
- Authors:
- Wang, Hui et al.
- Affiliation:
- Institute for Chemical Biology and Drug Discovery · United States
- Species:
- rodent
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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/26227776/