Compound ID | 3491

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MRS-2541

Class: Aminoacyl-tRNA synthetase inhibitor (methionyl tRNA synthetase [MetRS] inhibitor)

Spectrum of activity: Gram-positive
Details of activity: Active against methicillin-resistant and -susceptible Staphylococcus aureus, Enterococcus faecalis, vancomycin-resistant Enterococcus faecium, and Streptococcus pyogenes
Propensity to select resistant mutants: Yes, 10^-9 (low; comparable to ciprofloxacin Staphylococcus aureus resistance frequencey rate) at 4x and 8x MIC
Description: Synthetic compound; derived from MRS-2144; shows low mammalian cell line toxicity (safety margin by factor of 2 relative to MIC); shows comparable efficacy to linezolid when used in MRSA and Streptococcus infection in mice
Year first mentioned: 2024
Development status: Experimental
Chemical structure(s):
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Molecular weight: 473.29
Iso. SMILES: COC1=C(C=C(C(=C1)C2=C(N=CC3=NC(=CN32)CC4=NC5=C(N4)C=CC(=N5)Cl)F)Cl)OC
InChI Key: LBCDTMIQCKXLSS-UHFFFAOYSA-N
Can. SMILES: COC1=CC(=C(C=C1OC)Cl)C2=C(F)N=CC3=NC(=CN32)CC4=NC5=NC(=CC=C5N4)Cl
InChI: InChI=1S/C21H15Cl2FN6O2/c1-31-14-6-11(12(22)7-15(14)32-2)19-20(24)25-8-18-26-10(9-30(18)19)5-17-27-13-3-4-16(23)28-21(13)29-17/h3-4,6-9H,5H2,1-2H3,(H,27,28,29)
External links:
PubChem link: https://pubchem.ncbi.nlm.nih.gov/compound/172606457
Citation: https://journals.asm.org/doi/10.1128/aac.00745-24

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