Lusutrombopag

Class: Membrane-active agent

Spectrum of activity:	Gram-positive
Details of activity:	Active against vancomycin-resistant Enterococcus sp.; dissipates membrane potential
Description:	Synthetic compound; approved by FDA as a thrombopoietin receptor agonist; a repurposed drug; shows synergistic effect with aminoglycosides; no haemolytic activity observed; shows human cell line toxicity at 10xMIC; reduces bacterial load with tobramycin in murine peritonitis infection model with vancomycin-resistant Enterococcus
Institute where first reported:	Department of Laboratory Medicine, The Affiliated Changsha Hospital of Xiangya School of Medicine (The First Hospital of Changsha), Central South University, Changsha 410005, China
Year first mentioned:	2024
Development status:	Experimental

Chemical structure(s):
Canonical SMILES:	CCCCCCO[C@@H](C)C1=CC=CC(=C1OC)C2=CSC(=N2)NC(=O)C3=CC(=C(/C=C(\C)/C(=O)O)C(=C3)Cl)Cl
Isomeric SMILES:	CCCCCCO[C@@H](C)C1=CC=CC(=C1OC)C2=CSC(=N2)NC(=O)C3=CC(=C(C(=C3)Cl)/C=C(\C)/C(=O)O)Cl
InChI:	InChI=1S/C29H32Cl2N2O5S/c1-5-6-7-8-12-38-18(3)20-10-9-11-21(26(20)37-4)25-16-39-29(32-25)33-27(34)19-14-23(30)22(24(31)15-19)13-17(2)28(35)36/h9-11,13-16,18H,5-8,12H2,1-4H3,(H,35,36)(H,32,33,34)/b17-13+/t18-/m0/s1
InChI Key:	NOZIJMHMKORZBA-KJCUYJGMSA-N
Structure link:	https://pubchem.ncbi.nlm.nih.gov/compound/49843517

External links:
Guide to Pharmacology:	lusutrombopag
Main Source:	https://pubs.acs.org/doi/10.1021/acsinfecdis.3c00737