abstract |
NEW MATERIAL:A compound of formula I {R 1 and R 2 are each CH 3 or OCH 3 ; n is 0-21; m is 0 or 1; Z is of formula II [R 3 and R 4 are each H, (substituted) alkyl, etc.], formula III [R 5 is residue of α-amino acid or (substituted) glucosamine residue], formula IV (R 6 is 1-3C divalent hydrocarbon residue) or formula V}. n EXAMPLE: 3-(2,3-dimethoxy-5-methyl-1,4-benzoquinone-6-yl)propionylglycine. n USE: Medicines, protocollagen. Having proline hydroxylase-inhibitory effect and collagen biosynthesis-inhibitory effect, thus useful for the preventive/therapeutic agents for the organ fibrosis in mammals, antiallergic agents, etc. n PREPARATION: The carboxyl group of a compound of formula VI is converted to a reactive derivative, which is then reacted with a (substituted) α-amino acid of formula R 5 -H or (substituted) glucosamine in a solvent in the presence, if needed, of an organic base, thus obtaining the compound of the formula I (where, m is 0, Z is of formula III). n COPYRIGHT: (C)1991,JPO&Japio |