| 摘要 |
Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,5-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 5-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: <IMAGE> wherein: n is 1 or 0; R1 is hydrogen, lower alkyl, aryl or aralkyl; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl or aroyl; R5 is hydroxy, amino, or lower alkoxy; X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen; Y is hydrogen, lower alkyl, or aryl; R4 is -SH, <IMAGE> wherein L is O, NR7 or S (where R7 is hydrogen or lower alkyl); M is R8, OR8, SR8, or NR9R10 (where R8 is hydrogen, lower alkyl, aryl, or aralkyl; and R9 and R10 are, independently, hydrogen, lower alkyl, or aryl); A is O, NR15 or S; R11 and R12 are, independently, hydrogen, alkyl, aralkyl or aryl; R13 is hydrogen or lower alkyl; m is 0, 1, 2, or 3; R20 is hydrogen or aryl; and R21 is hydroxy or lower alkoxy; or pharmaceutically acceptable salts thereof.
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