THIAZOL-OXAZOLE MODIFIED PEPTIDES POSSESSING ABILITY TO INHIBIT BACTERIAL RIBOSOME Russian patent published in 2018 - IPC C07K14/26 A61P31/04 

FIELD: medicine; biotechnology.

SUBSTANCE: invention relates to the field of biotechnology and medicine, specifically to new thiazol-oxazole modified peptides that have the ability to inhibit the bacterial ribosome of E. coli, K. pneumoniae and Yersinia pseudotuberculosis by binding in its exit tunnel. Modified peptide has a general appearance NH2-Ser1-Gln2-Ser3-Pro4-Gly5-Asn6-Cys7-Ala8-Ser9-Cys10-Ser11-Asn12-Ser13-Pp-Ac with structure I, as represented in the claims, where NH₂ – N-terminal amide group, Ac – C-terminal acetyl group, Pp – polypeptide chain selected from ASANCTGGLG and KSANCTGGLG, and where the peptide contains a) three azole rings formed by Cys7, Cys10, Ser13 residues, and b) modification of the first two amino acids, resulting in the formation at the N-terminus of a 6-membered amidine ring molecule. Invention can be used as an antibacterial agent in medicine and experimental biology.

EFFECT: proposed peptides have an extensive ribosome binding site, far superior to that in the case of macrolide antibiotics, completely clog the exit tunnel of the ribosome and do not allow the newly synthesized peptides to overcome it.

1 cl, 4 dwg, 2 tbl