Lefamulin Chemical Properties

Boiling point:

618.6±55.0 °C(Predicted)

Density 

1.19±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMF: 16 mg/mL; DMSO: 12 mg/mL; Ethanol: 3 mg/mL; PBS (pH 7.2): 0.25 mg/mL

form 

A solid

pka

14.45±0.60(Predicted)

color 

White to off-white

InChIKey

KPVIXBKIJXZQJX-FCEONZPQSA-N

SMILES

C(O[C@@H]1C[C@](C=C)(C)[C@@H](O)[C@H](C)[C@@]23CC[C@@H](C)[C@]1(C)[C@]2([H])C(=O)CC3)(=O)CS[C@@H]1CC[C@@H](N)C[C@H]1O

Safety Information

WGK Germany 

WGK 3

Storage Class

11 - Combustible Solids

Hazard Classifications

STOT SE 2

Lefamulin Usage And Synthesis

Uses

Lefamulin is an antibiotic medication used in the treatment of adults with community-acquired bacterial pneumonia.

Biological Activity

Lefamulin inhibits bacterial protein synthesis by binding to the 50S subunit of the bacterial ribosome. Specifically, it binds to the peptidyl transferase center of the ribosome and inhibits the transfer of amino acids to growing polypeptide chains, which leads to the inhibition of bacterial protein synthesis and bacterial death. Lefamulin is active against a wide range of Gram-positive bacteria, including Streptococcus pneumoniae, Staphylococcus aureus, and methicillin-resistant S. aureus (MRSA), as well as some atypical bacteria such as Legionella species. It has also been shown to have activity against some Gram-negative bacteria, including Haemophilus influenzae and Moraxella catarrhalis.

Synthesis

synthesis route of Lefamulin

in vivo