| 摘要 |
PURPOSE:To provide a new dipeptide useful as a therapeutic agent for hypertension, bronchial asthma, etc., because of exhibiting an endothelin-antagonistic action and of inhibiting blood vessel contraction reactions caused by endothelin-1. CONSTITUTION:The compound of formula I [A is group of formula II n is 4-7), five or six-membered ring cycloalkyl; B is CO, CS, etc.; D is CHR<2> (R<2> is H, 1-6C alkyl), O; E is group of formula III or IV (R<3> is H, 1-4C alkyl; R<4> is 1-5C alkyl, aryl, etc.,); F is group of formula V or VI (R<5> is H, CHO, etc.,); G is group of formula VII (R<7> is nitrogen-containing aromatic heterocycle); Q is H, alkali metal, etc.,], e.g. N-[N-[2-(2- methylpropylidene)-3-(hexamethyleneiminocarbonyl)propionyl-N<1n>-methy l-D- tryptophan. The compound is produced by reacting a 2-alkylidenesuccinic acid anhydride with a cyclic amine of formula II, reducing the product, and subsequently reacting the produced 2-alkylsuccinic acid amide with D-TrP, D-TrP-D- TrP, etc. |
