| 摘要 |
<p>(A) (3-Aminopyrazine 2-carbonamido)guanidine 4-oxides (I) X = H, Cl, Br, CF3, alkoxy, alkyl, cycloalkyl, mononuclear aryl (opt. substd. by e.g. halogen, pref. Cl or Br), alkylmercapto, aralkylmercapto, alkylsulfonyl, aralkylsulfonyl, or dialkylamino R1 = H or acyl of formula R5 - CO - R5 = H, alkyl or aryl; R3 and R4 are each H, opt. branched (pref. normal) alkyl (opt. substd. by e.g. one or more hydroxyl, halogen, aryl (pref. phenyl opt. substd. by alkyl or halogen), amino (pref. a dialkylamino group in which the alkyl groups may be connected directly or via a heteroatom such as -O, forming a cyclic structure with the amino-N), cycloalkyl with 3-6 atoms in the ring, aryl (pref. mononuclear such as phenyl or substituted phenyl), amino or substituted amino, pref. a dialkylamino group. R3 + R4 may be both alkyl, connected directly or via a heteroatom and forming a cyclic structure with the N-atom esp. with 5-6 atoms in the ring, such as 1-pyrrolidinyl, piperidino or morpholino. (B) Pharmaceutically acceptable salts of (I) esp. the hydrochloride. The compounds have natriuretic properties. They differ from other effective diuretics because they promote the secretion of sodium selectively without increasing the secretion of potassium ions. They may be used in the treatment of oedema, hypertension and other diseases reacting to this treatment.</p> |
