| abstract |
An N-acylamino acid derivative of the formula: <IMAGE> (I) wherein each of R1, R2, R4 and R6 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms; each of R3 and R5 is hydrogen or lower alkyl; A is -CH(OH)-(CH2)qR7 wherein R7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a-monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms or -E-R10 wherein E is -S(O)i- wherein i is 0, 1 or 2, oxygen, -NR11- wherein R11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or <IMAGE> wherein each of R12 and R13 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R10 is hydrogen, i is 0, and a is an integer of from 0 to 5; or -CH2-CHR8-CO-R9 wherein R8 is hydrogen, lower alkyl, cycloalkyl, cycloalkylakyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms, and R9 is hydroxyl, -OX wherein, X is alkyl aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or -N(Y1)(Y2 ) wherein each of Y1and Y2is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y1 and Y2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hetero from; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R1 is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs. |