Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A
Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A
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DOI：
10.1016/j.bmcl.2004.07.097
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发表时间：
2004-12-20
影响因子：
2.7
通讯作者：
Scherkenbeck, J
中科院分区：
文献类型：
--
作者：
Dyker, H;Harder, A;Scherkenbeck, J
在驱虫环八缩酚肽 PF1022A (1) 中，二缩酚肽单元已替换为 β 转角模拟物 ((D))-Pro-((L))-Pro 和 BTD (7)，以阐明缩酚肽主链的功能作用。化合物 12 和 14 是第一个 PF1022A 类似物，其中 PF1022A 主链的大部分已被替换，从而改善了驱虫活性。初步的结构-活性关系表明对称构象是具有生物活性的构象。 (C) 2004 Elsevier Ltd. 保留所有权利。
In the anthelmintic cyclooctadepsipeptide PF1022A (1) didepsipeptide units have been exchanged for the beta-turn mimetics ((D))-Pro-((L))-Pro and BTD (7) in order to elucidate the functional role of the depsipeptide backbone. Compounds 12 and 14 are the first PF1022A analogues in which a substantial part of the PF1022A backbone has been replaced with an improvement of anthelmintical activity. Preliminary structure-activity relationships suggest a symmetric conformation to be the biological active one. (C) 2004 Elsevier Ltd. All rights reserved.