Compound ID | 668

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Actinonin (VRC483)

Class: Peptide deformylase inhibitor

Spectrum of activity: Gram-positive  &  Gram-negative
Details of activity: Peptide deformylase (PDF) inhibitors are growth inhibitors; bacterial static antibiotic for Gram positive bacteria, has activity against fastidious Gram negative bacteria. Active against S. aureus
Description: Margolis P, Hackbarth C, Lopez S, et al. Resistance to deformylase inhibitor VRC484 is caused by mutations in formyl transferase. 39th-ICAAC 1999;333.
Institute where first reported: Versicor (Pfizer, USA)
Year first mentioned: 1999
Highest developmental phase: Preclinical
Development status: Inactive
Reason Dropped: Actinonin was taken forward into clinical trials for other conditions including angiogenesis. Additionally resistance was in S. aureus was found to be at 10E-6 to 10E-7 with mutations in one gene required (1).
Chemical structure(s):
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Molecular weight: 385.5
Iso. SMILES: CCCCC[C@H](CC(=O)NO)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1CO
InChI Key: XJLATMLVMSFZBN-VYDXJSESSA-N
Can. SMILES: CCCCC[C@H](CC(=O)NO)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1CO
InChI: InChI=1S/C19H35N3O5/c1-4-5-6-8-14(11-16(24)21-27)18(25)20-17(13(2)3)19(26)22-10-7-9-15(22)12-23/h13-15,17,23,27H,4-12H2,1-3H3,(H,20,25)(H,21,24)/t14-,15+,17+/m1/s1
External links:
PubChem link: https://pubchem.ncbi.nlm.nih.gov/compound/443600
Citation: https://www.nature.com/articles/195701b0

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