Patent ID: 6355616
Filing Date: 2002-03-12
Classification: A61K,C07K

Abstract:
A compound with antifungal properties comprising a sequence having the formula:R1-leu-ile-gln-leu-R2 (SEQ ID NO: 60) wherein,R1 is selected from the group consisting of R3â€”, R3-&agr;-, and R3-&agr;-&khgr;-; R3 is selected from the group consisting of R4â€”CH2â€”, R4â€”CH2â€”COâ€”, R4â€”COâ€”, R4â€”SOyâ€”, and R4â€”POzâ€”; wherein, y=0-3, z=1-4; R4 is a hydrophobic moiety selected from the group consisting of a cyclic molecule having at least 3 carbon atoms, a heterocyclic molecule having at least 3 atoms, a functionalized cyclic molecule having at least 3 carbon atoms, and a functionalized heterocyclic molecule having at least three atoms; wherein said R4 is a hydrophobic moiety selected from the group consisting of biotin, 2-biphenylene, 2-anthraquinone, 2-benzofuran, 2-indole, 1-isoquinoline, hydroxyphenyl, 2-quinoline, 1-(3-(3,4-dihydroxycinnamoyl)-1,3,4,5-tetrahydroxycyclohexane), 1-(3,5-dichloro-2-hydroxyphenyl), 1-(3,5-diiodo-2-hydroxyphenyl), 1-(3,5-dinitro-2-hydroxyphenyl), 1-(4-azido-2-hydroxyphenyl), 4-biphenyl, 2-biphenyl, 1-naphthyl, 2-naphthyl, 3-amino-2-naphthyl, 3-chloro-2-nitrophenyl, (3,4-dihydroxyphenyl), 3,4,5-trihydroxyphenyl, 2-chloro-3-nitrophenyl, 5-azido-2-nitrophenyl, 3-amino-2-pyrazine, 2-benzyloxycarbonyl-ethyl, 2-thiophene, 2-(3,4-dihydroxyphenyl)ethene, 5-bromo-3-indolemethylene, 2-(4-hydroxy-3-methoxyphenyl)ethene, 2-(3-chlorophenyl)ethene, 2-pyrazine, 4-imidazole, 2-imino-1-imidazolidine, pyridine, 3-piperidine, 4-piperidine, fluorescein, 2-(4-amino-3,5,6-trichloro-pyridine), and 3-(2-chloro-6-fluorophenyl)-5-methylisoxazole; &agr; is a hydrophilic basic amino acid moiety selected from the group consisting of lysine, arginine, histidine, ornithine, diaminobutyric acid, citrulline, and para-amino phenylalanine; &khgr; is a hydrophobic amino acid moiety selected from the group consisting of alanine, naphthylalanine, biphenylalanine, valine, leucine, isoleucine, proline, hydroxyproline, phenylalanine, tryptophan, methionine, glycine, cyclohexylalanine, amino-isobutyric acid, norvaline, norleucine, tert-leucine, tetrahydroisoquinoline, pipecolic acid, phenylglycine, homophenylalanine, cyclohexylglycine, dehydroleucine, 2,2-diethylglycine, 1-amino-1-cyclopentane carboxylic acid, 1-amino-1-cyclohexane carboxylic acid, 2-amino-1-benzene carboxylic acid, 3-amino-1-benzene carboxylic acid, 3-amino-2-naphthene carboxylic acid, &ggr;-amino butyric acid, &bgr;-alanine, difluorophenylalanine, para-fluorophenylaniline, nipecotic acid, amino butyric acid, thienyl-alanine, and t-butyl-glycine; R2 is selected from the group consisting of â€”NH2, -&khgr;-NH2, -&khgr;-&agr;-NH2, -&khgr;-&agr;-&agr;-NH2, -&khgr;-&agr;-&agr;-&agr;-NH2,