Patent ID: 8188033
Filing Date: 2012-05-29
Classification: A61K,A61P,C07K,G16B

Abstract:
1. A synthetic antimicrobial peptide analog having a formula selected from the group consisting of: Σ-Glycine-O-(Tic-Oic-X-J-Tic-Oic-X—Z) Σ-Glycine-O-(Tic-Oic-X—Z-Tic-Oic-X-J) Σ-Glycine-B-(Tic-Oic-X—Z-Tic-Oic-X-J) Σ-Glycine-O-(Tic-Oic-X-J-Tic-Oic-X—Z) Σ-Glycine-O-(Tic-Oic-X—Z-Tic-Oic-X-J) Σ-Glycine-B-(Tic-Oic-X—Z-Tic-Oic-X-J) Σ-Glycine-O-(Tic-Oic-X-J-Tic-Oic-X—Z) Σ-Glycine-O-(Tic-Oic-X-J-Tic-Oic-X—Z) Σ-Glycine-O-(Tic-Oic-X-J-Tic-Oic-X—Z) Σ-Glycine-O-(Tic-Oic-X—Z-Tic-Oic-X-J) Σ-Glycine-O-(Tic-Oic-X—Z-Tic-Oic-X-J) Σ-Glycine-O-(Tic-Oic-Z-Tic-Oic-J) Σ-Glycine-B-(Tic-Oic-Z-Tic-Oic-J) Σ-Glycine-O-(Tic-Tic-X-J-Tic-Tic-X—Z) Σ-Glycine-O-(Tic-Tic-X—Z-Tic-Tic-X-J) Σ-Glycine-B-(Tic-Tic-X—Z-Tic-Tic-X-J) Σ-Glycine-O-(Tic-Tic-X-J-Tic-Tic-X—Z) Σ-Glycine-O-(Tic-Tic-X—Z-Tic-Tic-X-J) Σ-Glycine-B-(Tic-Tic-X—Z-Tic-Tic-X-J) Σ-Glycine-O-(Tic-Tic-X-J-Tic-Tic-X—Z) Σ-Glycine-O-(Tic-Tic-X-J-Tic-Tic-X—Z) Σ-Glycine-O-(Tic-Tic-X-J-Tic-Tic-X—Z) Σ-Glycine-O-(Tic-Tic-X—Z-Tic-Tic-X-J) Σ-Glycine-O-(Tic-Tic-X—Z-Tic-Tic-X-J) Σ-Glycine-O-(Tic-Tic-Z-Tic-Tic-J) Σ-Glycine-B-(Tic-Tic-Z-Tic-tic-J) Σ-Glycine-O-(Oic-Tic-X-J-Oic-Tic-X—Z) Σ-Glycine-O-(Oic-Tic-X—Z-Oic-Tic-X-J) Σ-Glycine-B-(Oic-Tic-X—Z-Oic-Tic-X-J) Σ-Glycine-O-(Oic-Tic-X-J-Oic-Tic-X—Z) Σ-Glycine-O-(Oic-Tic-X—Z-Oic-Tic-X-J) Σ-Glycine-B-(Oic-Tic-X—Z-Oic-Tic-X-J) Σ-Glycine-O-(Oic-Tic-X-J-Tic-Tic-X—Z) Σ-Glycine-O-(Oic-Tic-X-J-Oic-Tic-X—Z) Σ-Glycine-O-(Oic-Tic-X-J-Oic-Tic-X—Z) Σ-Glycine-O-(Oic-Tic-X—Z-Oic-Tic-X-J) Σ-Glycine-O-(Oic-Tic-X—Z-Oic-Tic-X-J) Σ-Glycine-O-(Oic-Tic-Z-Oic-Tic-J) Σ-Glycine-B-(Oic-Tic-Z-Oic-tic-J) Σ-Glycine-O-(Oic-Oic-X-J-Oic-Oic-X—Z) Σ-Glycine-O-(Oic-Oic-X—Z-Oic-Oic-X-J) Σ-Glycine-B-(Oic-Oic-X—Z-Oic-Oic-X-J) Σ-Glycine-O-(Oic-Oic-X-J-Oic-Oic-X—Z) Σ-Glycine-O-(Oic-Oic-X—Z-Oic-Oic-X-J) Σ-Glycine-B-(Oic-Oic-X—Z-Oic-Oic-X-J) Σ-Glycine-O-(Oic-Oic-X-J-Oic-Oic-X—Z) Σ-Glycine-O-(Oic-Oic-X-J-Oic-Oic-X—Z) Σ-Glycine-O-(Oic-Oic-X-J-Oic-Oic-X—Z) Σ-Glycine-O-(Oic-Oic-X—Z-Oic-Oic-X-J) Σ-Glycine-O-(Oic-Oic-X—Z-Oic-Oic-X-J) Σ-Glycine-O-(Oic-Oic-Z-Oic-Oic-J) Σ-Glycine-B-(Oic-Oic-Z-Oic-tic-J) Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U Σ-U wherein Tic stands for tetrahydroisoquinolinecarboxylic acid, Oic stands for octahydroindolecarboxylic acid, Σ is acetyl, NH U is lysine, arginine, histidine, ornithine, 2,3-diaminopropionic acid (Dpr), diaminobutanoic acid (Dab), 4-aminopiperidine-4-carboxylic acid (Apc4), or 3-aminopiperidine-3-carboxylic acid (Apc3), X is glycine, alanine, β-alanine, gamma-aminobutyric acid (Gaba), ∈-aminohexanoic acid (Ahx), phenylglycine (Phg), 9-aminooctanoic acid (9-Aoa), 10-aminodecanoic acid (10Ada), 12-aminododecanoic acid (12-Adda), or 16-aminopalmitic acid (16-Apa), J is lysine, arginine, histidine, ornithine, 2,3-diaminopropionic acid (Dpr), or 2,4-diaminobutanoic acid (Dab), Z is phenylalanine, tyrosine, tryptophan, 4-fluorophenylalanine (Fpa), 4-chlorophenylalanine (Cph), 4-nitrophenylalanine (Nph), phenyl glycine (Phg), valine, isoleucine, norvaline, norleucine, norisoleucine, 4-Aminobutyric acid, piperidinic acid, 6-Aminocaproic acid, 2-Aminoheptanoic acid, 2-Aminoisobutyric acid, 3-Aminoisobutyric acid, 2-Aminopimelic acid, 2,4-Diaminobutyric acid, N-Ethylglycine, allo-Isoleucine, N-Methylglycine, N-Methylisoleucine, or N-Methylvaline, O is phenylalanine, leucine, valine or isoleucine, B is lysine, arginine, histidine, ornithine, 2,3-diaminopropionic acid (Dpr), 2,4-diaminobutanoic acid (Dab), 4-aminopiperidine-4-carboxylic acid (Apc4), or 3-aminopiperidine-3-carboxylic acid (Apc3), Π is glycine, alanine, β-alanine, gamma-aminobutyric acid (Gaba), or ∈-Aminohexanoic acid (Ahx), n is 1 to 4 repeating units, m is 1 to 5 repeating units, and k is 1 to 5 repeating units.