Solid‐Phase Total Synthesis and Antimicrobial Activities of Loloatins A–D
Solid‐Phase Total Synthesis and Antimicrobial Activities of Loloatins A–D
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DOI：
10.1002/cbdv.200790232
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发表时间：
2007-12
影响因子：
2.9
通讯作者：
Yan Ding;Chuanguang Qin;Zhihong Guo;W. Niu;Ruijie Zhang;Yang Li
中科院分区：
文献类型：
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作者：
Yan Ding;Chuanguang Qin;Zhihong Guo;W. Niu;Ruijie Zhang;Yang Li
十肽抗生素 Loloatins A–D (1–4) 的首次全合成最初是从海洋细菌分离株 MK-PNG-276A（可能属于芽孢杆菌属）中分离出来的，通过固相肽合成 (SPPS) 完成，然后在安全捕获树脂上对活化的线性前体进行“头尾”环化，不保护亲核侧链功能。合成肽与从细菌来源分离的天然产物具有同样的活性，并且被发现与两亲性抗菌环十肽家族中的其他成员具有相似的细菌选择性。
The first total synthesis of the decapeptide antibiotics loloatins A–D (1–4), originally isolated from the marine bacterial isolate MK‐PNG‐276A, possibly in the genus Bacillus, was accomplished by solid‐phase peptide synthesis (SPPS), followed by ‘head‐to‐tail’ cyclization of the activated linear precursors, without protection of nucleophilic side‐chain functions, on a safety‐catch resin. The synthetic peptides were equally active as the natural products isolated from the bacterial source and found to possess similar bacterial selectivity as other members in the family of amphipathic antimicrobial cyclic decapeptides.