| 摘要 |
<p>Analgesic and hypotensive activity is exhibited by compounds having the formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="11" wi="85" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>and pharmaceutically acceptable salts thereof, wherein</p><p>R, 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;</p><p>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, or
<Chemistry id="chema02" num="0002"><Image id="ia02" he="13" wi="29" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>
wherein n<Sub>6</Sub> is an integer of 2 to 15;</p><p>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; and</p><p>n<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.</p> |
