N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
复制标题
N-苄基焦谷氨酰-L-苯丙氨酸衍生物作为 VCAM/VLA-4 拮抗剂。
DOI：
10.1016/s0960-894x(00)00089-5
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发表时间：
2000
影响因子：
2.7
通讯作者：
K. Rowan
中科院分区：
文献类型：
--
作者：
L. Chen;J. Tilley;R. Guthrie;F. Mennona;T. N. Huang;G. Kaplan;R. Trilles;D. Miklowski;N. Huby;V. Schwinge;B. Wolitzky;K. Rowan
制备了一系列N-(N-苄基焦谷氨酰)-4-取代-1-苯丙氨酸衍生物作为VLA-4/VCAM拮抗剂。被带有大量邻位取代基的缺电子苯甲酰氨基取代的类似物在 ELISA 测定中具有低 nM 效力，在基于细胞的测定中具有低 μM 活性。
A series of N-(N-benzylpyroglutamyl)-4-substituted-l-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA assay and low-μM activity in a cell based assay.