| 摘要 |
A series of cationic cyclic peptides, useful for the treatment of infectious diseases in both human and veterinary clinical/surgical environment are described herein. The peptides of the invention have a length of 15 to 21 amino acids, and show a sequence A-B-C-D-C′-B′-A′, wherein units A and A′ correspond to —NH2 terminal and —COOH terminal regions; units B and B′ correspond to cyclizable amino acids containing sulfur; units C and C are sequences of 5 amino acids selected among hydrophobic amino acids, basic amino acids and amino acids forming hydrogen bonds; unit D is a dipeptide consisting of glycine and one basic amino acid. Said peptides show significant antibacterial activity, associated with high stability and resistance to the action of bacterial endopeptidases, and weak or null toxicity against eukaryotic cells. |
| 主权项 |
1. Peptide having a sequence A-B-C-D-C′-B′-A′, wherein: each unit A consists independently of 1-3 amino acids; each unit B consists independently of an amino acid containing sulfur; each unit C consists independently of 5 amino acids, selected both in group (a) of hydrophobic amino acids, and in group (b) of basic amino acids or amino acids forming hydrogen bonds; unit D consists of glycine, and one basic amino acid,
wherein: (i) said hydrophobic amino acids are selected from: Ala, Phe, Ileu, Leu, Pro, Tyr, Trp and Val; (ii) said basic amino acids are selected from: Lys, His, Arg; (iii) said amino acids forming hydrogen bonds are selected from Asn, Gln, Ser, Thr; and wherein the substructure C-D-C′ as a whole contains 5 to 9 points of alternation between amino acid of group (a) and amino acid of group (b), or vice versa. |
