AMINOTHIOLPEPTIDE.

摘要

Analgesic and hypotensive activity is exhibited by compounds having the formula +TR (A1)n1(A2)n2(A3)n3(A4)n4(A5)n5R3, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl; R3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy, or -NY1Y2, wherein Y1 and Y2 are each independently hydrogen, alkyl, aryl, or arylalkyl, or Y1 is hydrogen and Y2 is substituted alkyl or (heteroaryl)alkyl; A1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or wherein n6 is an integer of 2 to 15; A2, A3, A4 and A5 each is independently glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, or norvalyl; and n1, n2, n3, n4 and n5 each is independently 0 or 1.