| 摘要 |
Pentapeptides (I) - (VI), containing a cyclohexane ring (or oxa, thia, selena, aza or phospha analog) in the peptide chain, and their salts are new. Peptides of formulae (I) - (VI) and their salts are new. y<1>-A-B'-C'-D-Z-y<2> (I) y<1>-Z-A-B'-C'-D-y<2> (II) y<1>-D-Z-A-B'-C'-y<2> (III) y<1>-C'-D-Z-A-B'-y<2> (IV) y<1>-B'-C'-D-Z-A-y<2> (V) Z = aminoacid residue containing a 5-membered ring, of formula (i); X = O, S, Se, NR9, PR9 or CR9R10; R9, R10 = H, OH, SH or halo; or alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, alkoxy, alkenyloxy, aryloxy, alkylthio, arylthio, alkylseleno or arylseleno (optionally substituted (os) by F, OH, SH, SeH, NH2, =O or COOH); Q1, Q2 = direct bond, CH2, CH(OH), CH(OR1), CHR1 or CR1R2; R1, R2 = alkyl, alkenyl, aryl, alkaryl or aralkyl (os by F, OH, NH2 or COOH); Q3 - Q8 = direct bond, O, S, Se, N2, NR9 or PO3; R3 - R8 = H, OH, SH, N3, CN, NC, SCN, halo, SO3, NO2, PR11R12 or COOR11; or alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, alkanoyl, alkenoyl, alkynoyl, aroyl, aralkanoyl or alkaroyl (os by F, OH, SH, SeH, NH2, =O or COOH); or two of R3 - R8 together = group completing a 5- or 6-membered ring (os by 1 or 2 of alkyl, alkenyl and aryl); R11, R12 = H, OH, SH, halo, CN, NC or SCN; or alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, alkoxy, alkenyloxy, aryloxy, alkylthio, alkenylthio, arylthio, alkylseleno, arylseleno, aralkanoyloxy, aralkanoyloxy, aralkoxy or alkaryloxy (os by F, OH, SH, SeH, NH2, =O or COOH); A = alpha -, beta - or psi -aminoacid with an aromatic or aliphatic side-chain; B' = alpha -, beta - or psi -aminoacid with an aromatic side-chain; C' = alpha -, beta - or psi -aminoacid with a basic or aliphatic side-chain; D = alpha -, beta - or psi -aminoacid with a side-chain containing no acidic or basic groups; y1 = H, CH3(CH2)rCO, butoxycarbnyl or 9-fluorenylmethoxycarbonyl; r = 0-6; and y2 = H, NH2, alkoxy, aryloxy, alkyl, aryl, alkenyl, alkynyl, halo, CN, NC, SCN, alkylthio or arylthio. A, B', C', D and Z are bonded to each other via peptide groups; y1 is bonded to the amino group of the corresponding aminoacid; and y2 is bonded to the carboxy group of the corresponding aminoacid. An Independent claim is included for the preparation of (I).
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