Synthetic study of VLA-4/VCAM-1 inhibitors: Synthesis and structure–activity relationship of piperazinylphenylalanine derivatives
作者： Osamu Saku , Kiminori Ohta , Eri Arai , Yuji Nomoto , Hiroko Miura
DOI: 10.1016/J.BMCL.2007.12.014
关键词:
摘要: To improve the poor pharmacokinetic characteristics of VLA-4 inhibitors, novel piperazinylphenylalanine derivatives were designed. This structure is expected to physicochemical properties by increasing overall basicity. By changing components at 4-position piperazine and terminal group amido bond, 12t was found be most potent this series compounds. In addition, dichlorobenzoyl derivative 12aa exhibited better oral availability showed efficacy in an vivo model after administration.
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