摘要 |
<p>PURPOSE: To obtain an indole-containing peptide having an excellent neutral metalloendopeptidase-inhibiting action and useful as an antihypertensive agent, a diuretic agent and/or a cardiac failure or renal insufficiency-preventing or therapeutic agent. CONSTITUTION: A compound of formula I (R is H, lower alkyl, formyl; X is O,S), its ester or their pharmacologically acceptable salts, e.g. 4- carboxy-5- 2-[N-((1S)-1-carboxy-2-(3-indolyl)ethyl)-(L)-phenylalanyl] aminoethyl} oxazole. The compound is obtained by condensing a carboxylic acid compound of formula II (R<1> is a carboxyl-protecting group) or its salt with an amine compound of formula III (R<2> is a carboxyl-protecting group) or its salt in the presence of a dehydrating agent by a conventional peptide-synthesizing method. The compound is useful as an agent for preventing and treating congestive heart failure, pulmonary edema, hepatic edema, hepatic hydrocele, ascites disease, and interstitial nephritis or as a hypertension-treating agent.</p> |