Antimicrobial hexapeptides

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/06 (2006.01) A61K 38/08 (2006.01) A61P 31/00 (2006.01)

Patent

CA 2597191

The invention encompasses hexapeptides consisting of alternating hydrophobic residues (B) at positions 2, 4, and 6, hydrophilic, hydrophilic, charged residues (X) at positions 1 and 3, and a naphthylalanine (NaI), an aliphatic or aromatic residue (O) at position five, represented generally by the formula XBXBOB, which exhibit antimicrobial activity against infections caused by a variety of pathogens. These pathogens may include gram positive or negative bacteria, acid-fast bacteria such a mycobacteria, parasites, dermatophytes, or fungal pathogens. Typical fungal pathogens include Candida albicans and typical dermatophytes include Trichophyton rubrum and Trichophyton mentagrophytes. The hexapeptides of the present invention exhibit antifungal activity, antibacterial activity, desirable stability, and lack toxicity to the mammal receiving treatment.

La présente invention a trait à des hexapeptides constitués de résidus (B) hydrophobes aux positions 2, 4, et 6, de résidus (X) chargés hydrophiles aux positions 1 et 3, et une naphtylalanine (Nal), un résidu (O) aliphatique ou aromatique à la position 5, représentés par la formule générale XBXBOB, présentant une activité antimicrobienne contre des infections provoquées par divers agents pathogènes. Ces agents pathogènes peuvent inclure des bactéries Gram positif ou négatif, des bactéries acidorésistantes telles que des mycobactéries, des parasites, des dermatophytes, ou des agents pathogènes fongiques. Des agents pathogènes fongiques typiques comprennent Candida albicans et des dermatophytes typiques comprennent Trichophyton rubrum et Trichophyton mentagrophytes. Les hexapeptides de la présente invention présentent une activité antifongique, une activité antibactérienne, une stabilité souhaitable, et ne sont pas toxiques vis-à-vis d'un mammifère sous traitement.

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