Chemistry:TP0586532
From HandWiki
TP0586532 is an experimental antibiotic drug, which acts as a potent and selective inhibitor of the bacterial enzyme UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC). This enzyme is important for the production of Lipid A, a key component of the cell membrane of Gram-negative bacteria. Previous inhibitors of LpxC have failed to progress into clinical trials in humans, mostly because of off-target cardiovascular toxicity, so TP0586532 was based on a different structural class which is hoped to reduce this risk. In animal studies it shows activity against carbapenem-resistant Klebsiella pneumoniae but has not yet progressed into human trials.[1][2][3]
See also
References
- ↑ "Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532". Bioorganic & Medicinal Chemistry 30. January 2021. doi:10.1016/j.bmc.2020.115964. PMID 33385955.
- ↑ "Pharmacodynamic target assessment and prediction of clinically effective dosing regimen of TP0586532, a novel non-hydroxamate LpxC inhibitor, using a murine lung infection model". Journal of Infection and Chemotherapy 28 (5): 635–642. May 2022. doi:10.1016/j.jiac.2022.01.004. PMID 35131156.
- ↑ "TP0586532, a non-hydroxamate LpxC inhibitor, has in vitro and in vivo antibacterial activities against Enterobacteriaceae". The Journal of Antibiotics 75 (2): 98–107. February 2022. doi:10.1038/s41429-021-00486-3. PMID 34837061.
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