Lolamicin

Class: Lipoprotein transport system inhibitor (LolCDE inhibitor)

Spectrum of activity:	Gram-negative
Details of activity:	Active against Escherichia coli, Salmonella typhimurium, Klebsiella pneumoniae, and Enterobacter cloacae, but not active against Gram-positives; targets the lipoprotein transport system
Description:	Synthetic compound; derived by combining pyridinepyrazole and pyridineimidazole and further modified to improve accumulation in Gram-negative; shows no activity against Gram-negative gut commensals; reduces bacterial burden by 3-log when administered orally in mice infected with colistin-resistant Escherichia coli; no activity against
Year first mentioned:	2024
Development status:	Experimental

Chemical structure(s):
Canonical SMILES:	CC1=NC(=CC(=C1)C2=C(C3=CC(=CC=C3)OCC4=CC(=CC=C4)C#N)NN=C2)C
Isomeric SMILES:	CC1=NC(=CC(=C1)C2=C(C3=CC(=CC=C3)OCC4=CC(=CC=C4)C#N)NN=C2)C
InChI:	InChI=1S/C24H20N4O/c1-16-9-21(10-17(2)27-16)23-14-26-28-24(23)20-7-4-8-22(12-20)29-15-19-6-3-5-18(11-19)13-25/h3-12,14H,15H2,1-2H3,(H,26,28)
InChI Key:	CIXIQLLJOWEAKU-UHFFFAOYSA-N

External links:
Guide to Pharmacology:	lolamicin
Main Source:	https://www.nature.com/articles/s41586-024-07502-0