Varnavas A, Valenta V, Berti F, Lassiani L
Department of Pharmaceutical Sciences, University of Trieste, Italy.
Farmaco. 2001 Aug;56(8):555-64. doi: 10.1016/s0014-827x(01)01071-0.
A series of new N-substituted anthranilic acid dimer derivatives having a C-terminal Phe residue was synthesized and evaluated for their affinity for CCK receptors. These compounds resulted from a blended approach based firstly on the use of an alternative substructure embedded within asperlicin and secondly on the derivatization of this template with substituents chosen considering the C-terminal primary structure of the endogenous ligand. Although these compounds exhibited a regnylogical-type organization similar to that of CCK-4, they are characterized by about 1000-fold greater affinity for CCK-A receptor than the C-terminal tetrapeptide.
合成了一系列具有C端苯丙氨酸残基的新型N-取代邻氨基苯甲酸二聚体衍生物，并对其与CCK受体的亲和力进行了评估。这些化合物是通过一种混合方法得到的，该方法首先基于使用嵌入asperlicin中的替代亚结构，其次基于用考虑内源性配体C端一级结构选择的取代基对该模板进行衍生化。尽管这些化合物表现出与CCK-4类似的受体结合类型组织，但它们对CCK-A受体的亲和力比C端四肽高约1000倍。
