后他汀，一种脯氨酰内肽酶的新型抑制剂。VI. 含吡咯烷环的后他汀类似物的内肽酶抑制活性。
Poststatin, a new inhibitor of prolyl endopeptidase. VI. Endopeptidase inhibitory activity of poststatin analogues containing pyrrolidine ring.
作者信息
Tsuda M, Muraoka Y, Someno T, Nagai M, Aoyagi T, Takeuchi T
机构信息
Institute of Microbial Chemistry, Tokyo, Japan.
出版信息
J Antibiot (Tokyo). 1996 Sep;49(9):900-8. doi: 10.7164/antibiotics.49.900.
Several pyrrolidine-containing analogues of poststatin were synthesized and examined for their inhibitory activity against prolyl endopeptidase and cathepsin B in vitro. Replacement of the postine residue with 2-oxo-2-(2-pyrrolidinyl)acetic acid increased the selectivity and inhibitory activity against prolyl endopeptidase. Benzyloxycarbonyl-L-phenylalanyl-(S)-2-oxo-2- (2-pyrrolidinyl)acetyl-D-phenylalanine was about 46 times as active to propyl endopeptidase as natural poststatin.
合成了几种含吡咯烷的poststatin类似物，并在体外检测了它们对脯氨酰内肽酶和组织蛋白酶B的抑制活性。用2-氧代-2-(2-吡咯烷基)乙酸取代postine残基提高了对脯氨酰内肽酶的选择性和抑制活性。苄氧羰基-L-苯丙氨酰-(S)-2-氧代-2-(2-吡咯烷基)乙酰-D-苯丙氨酸对脯氨酰内肽酶的活性约为天然poststatin的46倍。
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