Turk J, Needleman P, Marshall G R
J Med Chem. 1975 Nov;18(11):1135-9. doi: 10.1021/jm00245a018.
Three analogs of bradykinin have been synthesized which bear a bromoacetyl function on the alpha-amino group or on an anilinic amino group at position 5 or 8. It was hoped that one or more of these analogs might act as an irreversible bradykinin antagonist or as a long-acting converting enzyme inhibitor. Although none of the analogs exhibited the desired pharmacological properties, the methods described for the synthesis and characterization of peptides bearing anilinic bromoacetyl groups are of potential utility in the development of antagonists of other tyrosine--or phenylalanine--containing peptides.
已合成了三种缓激肽类似物,它们在α-氨基上或5位或8位的苯胺基氨基上带有溴乙酰基官能团。人们希望这些类似物中的一种或多种可能作为不可逆的缓激肽拮抗剂或长效转化酶抑制剂起作用。尽管这些类似物均未表现出所需的药理特性,但所描述的用于合成和表征带有苯胺基溴乙酰基的肽的方法在开发其他含酪氨酸或苯丙氨酸的肽的拮抗剂方面具有潜在的实用性。