Solid-phase synthesis and biological activity of malformin C and its derivatives
Solid-phase synthesis and biological activity of malformin C and its derivatives
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DOI：
10.1038/ja.2009.100
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发表时间：
2009-12-01
影响因子：
3.3
通讯作者：
Omura, Satoshi
中科院分区：
文献类型：
--
作者：
Kojima, Yasuhiro;Sunazuka, Toshiaki;Omura, Satoshi
我们完成了适合于各种衍生物的制备的固相全合成。通过树脂上的大乳糖化和二硫键的形成，同时从树脂上裂解，实现了马福林C的固相全合成。抗疟疾和抗锥虫活性被检测，这有助于阐明部分结构-活性关系。结果表明，二硫键是必需的，支链氨基酸也是关键成分，如果化合物要表现出有效的抗疟疾和抗锥虫特性。《抗生素杂志》(2009年)62681686；doi：10.1038/ja.2009.100；10月30日在线发布
We accomplished the solid-phase total synthesis of malformin C, which is adaptable for the easy preparation of various derivatives. A solid-phase total synthesis of malformin C was achieved by on-resin macrolactannization and disulfide bond formation, with concurrent cleavage from the resin. Antimalarial and antitrypanosomal activities were examined, which helped elucidate partial structure-activity relationships. Results indicate that the disulfide bond is essential and branched amino acids are also crucial components if the compound is to exhibit potent antimalarial and antitrypanosomal properties. The Journal of Antibiotics (2009) 62, 681-686; doi:10.1038/ja.2009.100; published online 30 October 2009