丁香实验_LOGO
登录
提问
我要登录
|免费注册
点赞
收藏
wx-share
分享

(E)-Alkene Peptide Bond Isosteres by Cuprate Opening of Vinyl Aziridines

互联网

726
Alkene isosteres are important nonhydrolyzable and rigidified analogs of peptide bonds. The ( E -alkene effectively mimics the three-dimensional structure of the amide bond, especially the C(α) n −C(α) n+1 distance (Fig. 1 ). The incorporation of an alkene isostere into a biologically active peptide provides a peptidomimetic that should have improved resistance to proteolysis and similar conformational preferences. The low polarity of the alkene is useful in increasing lipophilicity, but hydrogen bonding or dipolar interactions are generally not possible.
 
Fig. 1.  Geometry of peptide bond and alkene isostere.

提问
扫一扫
丁香实验小程序二维码
实验小助手
丁香实验公众号二维码
扫码领资料
反馈
TOP
打开小程序