Summary information and primary citation
- PDB-id
- 4ioa; SNAP-derived features in text and JSON formats;
DNAproDB
- Class
- ribosome-ribosome inhibitor
- Method
- X-ray (3.2 Å)
- Summary
- Crystal structure of compound 4e bound to large ribosomal subunit (50s) from deinococcus radiodurans
- Reference
- Magee TV, Han S, McCurdy SP, Nguyen TT, Granskog K, Marr ES, Maguire BA, Huband MD, Chen JM, Subashi TA, Shanmugasundaram V (2013): "Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates." Bioorg.Med.Chem.Lett., 23, 1727-1731. doi: 10.1016/j.bmcl.2013.01.067.
- Abstract
- A novel series of 3-O-carbamoyl erythromycin A derived analogs, labeled carbamolides, with activity versus resistant bacterial isolates of staphylococci (including macrolide and oxazolidinone resistant strains) and streptococci are reported. An (R)-2-aryl substituent on a pyrrolidine carbamate appeared to be critical for achieving potency against resistant strains. Crystal structures showed a distinct aromatic interaction between the (R)-2-aryl (3-pyridyl for 4d) substituent on the pyrrolidine and G2484 (G2505, Escherichia coli) of the Deinococcus radiodurans 50S ribosome (3.2Å resolution).
