| abstract |
Analgesic and hypotensive activity is exhibited by compounds having the formulaand pharmaceutically acceptable salts thereof, whereinR, and R<sub>2</sub> are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (hetero aryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R<sub>3</sub> is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy, or -NY<sub>1</sub>Y<sub>2</sub>, wherein Y, and Y<sub>2</sub> are each independently hydrogen, alkyl, aryl, or arylalkyl, or Y, is hydrogen and Y<sub>2</sub> is substituted alkyl or (heteroaryl)alkyl; A<sub>1</sub> is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, orwherein n<sub>6</sub> is an integer of 2 to 15;A<sub>2</sub>, A<sub>3</sub>, A<sub>4</sub> and A<sub>5</sub> 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; andn<sub>1</sub>, n<sub>2</sub>, n<sub>3</sub>, n<sub>4</sub> and n<sub>s</sub> each is independently 0 or 1. |