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1. WO2020065595 - SHORT LEOPEPTIDES WITH ANTIMICROBIAL ACTIVITY AGAINST GRAM NEGATIVE AND GRAM POSITIVE BACTERIA

Publication Number WO/2020/065595
Publication Date 02.04.2020
International Application No. PCT/IB2019/058204
International Filing Date 27.09.2019
IPC
C07K 4/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
4Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
A61P 31/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
CPC
A61K 38/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C07K 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
C07K 4/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
4Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
Applicants
  • UNIVERSIDAD NACIONAL DE COLOMBIA [CO]/[CO]
Inventors
  • ORDUZ PERALTA, Sergio
  • POSADA TABARES, Vanessa
  • ESPEJO BENAVIDES, Blanca Fabiola
Agents
  • PACANCHIQUE VARGAS, Rubiela
Priority Data
NC2018/001043028.09.2018CO
Publication Language Spanish (ES)
Filing Language Spanish (ES)
Designated States
Title
(EN) SHORT LEOPEPTIDES WITH ANTIMICROBIAL ACTIVITY AGAINST GRAM NEGATIVE AND GRAM POSITIVE BACTERIA
(ES) LIPOPEPTIDOS CORTOS CON ACTIVIDAD ANTIMICROBIANA CONTRA BACTERIAS GRAM NEGATIVAS Y GRAM POSITIVAS
(FR) LIPOPEPTIDES COURTS À ACTIVITÉ ANTIMICROBIENNE CONTRE DES BACTÉRIES À GRAM NÉGATIF ET À GRAM POSITIF
Abstract
(EN)
The present invention relates to synthetic leopeptides of formula Cn-X1-X2-X3-NH2 , wherein: Cn is a fatty acid selected from the group consisting of C12 to C16; X1 is at least one glycine molecule; X2 is at least two natural amino acids that have a positive net charge and/or are not proteinogenic; and X3 can be present or absent, and when it is present it is at least one aliphatic amino acid. The lipopeptides have antimicrobial activity against pathogenic bacteria (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii, Serratia marcescens, Staphylococcus saprophyticus, Staphylococcus haemolyticus and Streptococcus salivarius), at minimum inhibitory concentrations (MIC) between 8 and 50 µM. In addition, they do not display toxicity in human red blood cells or in mosquito larvae in concentrations between 3.13 and 50.0 µM at an evaluated concentration of 100 µM.
(ES)
La presente invención se refiere a lipopéptidos sintéticos de fórmula Cn-X1-X2-X3-NH2 en donde: Cn es un ácido graso seleccionado del grupo que consiste de C12 a C16; X1 es al menos una molécula de glicina; X2 es al menos dos aminoácidos naturales con carga neta positiva y/o no proteinogénicos; y, X3 puede estar presente o ausente y cuando está presente es al menos un aminoácido alifático, Los lipopéptidos presentan actividad antibacteriana contra bacterias patógenas (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii, Serratia marcescens, Staphylococcus saprophyticus, Staphylococcus haemolyticus y Streptococcus salivarius) a concentraciones mínimas inhibitorias (CMI) entre 8 a 50 µM. Adicionalmente, no presentaron toxicidad en eritrocitos humanos ni en larvas de mosquito en concentraciones entre 3,13 y 50,0 µM a una concentración evaluada de 100 µM.
(FR)
La présente invention concerne des lipopeptides synthétiques de formule Cn-X1-X2-X3-NH2 dans laquelle: Cn est un acide gras sélectionné dans le groupe constitué de C12 à C16; X1 est au moins une molécule de glycine; X2 est au moins deux aminoacides naturels avec charge nette positive et/ou non protéinogènes; et, X3 peut être présent ou absent et lorsqu'il est présent il est au moins un aminoacide aliphatique. Les lipopeptides présentent une activité antibactérienne contre les bactéries pathogènes (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii, Serratia marcescens, Staphylococcus saprophyticus, Staphylococcus haemolyticus y Streptococcus salivarius) dans des concentrations minimales inhibitrices (CMI) entre 8 et 50 µM. En outre, ils ne sont pas toxiques pour les érythrocytes humains ni pour les larves de moustique dans des concentrations entre 3,13 et 50,0 µM à une concentration évaluée à 100 µM.
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