Argifin efficient solid phase total synthesis and evaluation of analogues of acyclic peptide
Argifin efficient solid phase total synthesis and evaluation of analogues of acyclic peptide
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Argifin无环肽类似物的高效固相全合成及评价
DOI：
10.1016/j.bmc.2009.02.047
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发表时间：
2009
期刊：
影响因子：
--
通讯作者：
Satoshi. mura.
中科院分区：
文献类型：
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作者：
Toshiaki Sunazuka;Akihiro Sugawara;Kanami Iguchi;Tomoyasu Hirose;Kenichiro Nagai;Yoshihiko Noguchi;Yoshifumi Saito;Tsuyoshi Yamamoto;Hideaki Ui;Hiroaki Gouda;Kazuro Shiomi;Takeshi Watanabe;Satoshi. mura.
开发了一种有效的固相合成精氨酸，为后续有效合成类似物提供了途径，总收率为13%，并阐明了结构-活性关系。从精氨酸的合成中间体中制备的新的无环肽18b被发现对粘质沙雷氏菌几丁质酶B的抑制作用是精氨酸本身的70倍
An effective solid phase synthesis of Argifin, providing subsequent access to effective synthesis of analogues, was developed in 13% overall yield, as well as elucidating structure–activity relationships. The novel acyclic peptide 18b, prepared from a synthetic intermediate of Argifin, was found to be 70 times more potent as an inhibitor of Serratia marcescens chitinases B than Argifin itself