Bioorganic chemistry

Synthesis of a novel cyclic prodrug of RGD peptidomimetic to improve its cell membrane permeation

X Song, CR Xu, HT He, TJ Siahaan

文献索引：Song, Xiaoping; Xu, Christine R.; He, Henry T.; Siahaan, Teruna J. Bioorganic Chemistry, 2002 , vol. 30, # 4 p. 285 - 301

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被引用次数: 23

摘要

The objective of this work was to synthesize cyclic prodrug 2 derived from the parent RGD peptidomimetic 1 and to evaluate its chemical and enzymatic stabilities and antithrombic activity. Cyclic prodrug 2 was formed to improve the cell membrane permeation of RGD peptidomimetic 1 by transiently masking the unfavorable physicochemical properties of compound 1. Cyclic prodrug 2 was synthesized by linking the amino and carboxylic acid ...