84827-40-7Relevant articles and documents
N-substituted-amido-amino acids
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, (2008/06/13)
Compounds of the formula STR1 wherein R and R9 are independently hydroxy or lower alkoxy, R1 and R2 are hydrogen or lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6
Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives
Stanton,Gruenfeld,Babiarz,Ackerman,Friedmann,Yuan,Macchia
, p. 1267 - 1277 (2007/10/02)
The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x), -N-arylalanines (15a,b), -N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure-activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 x 10-9 M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.
