Analogues of both Leu- and Met-enkephalin containing a constrained dipeptide isostere prepared from a Baylis-Hillman adduct

Roberta Galeazzi; Gianluca Martelli; Eleonora Marcucci

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Analogues of both Leu- and Met-enkephalin containing a constrained dipeptide isostere prepared from a Baylis-Hillman adduct

机译：由Baylis-Hillman加合物制备的含有受约束的二肽等排物的Leu-和Met-脑啡肽的类似物

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摘要

An efficient route was developed for the synthesis of the Fmoc-protected dipeptide 4, isostere of Gly-Gly containing an α-methylene β-amino acid; the conformationally reitricted analogues of Leu-enkephalin, 3a, and Met-enkephalin, 3b, respectively, were prepared by changing 4 for Gly~2-Gly~3 in the native compounds 3a and 3b whose biological activities were significantly lower than the parent compounds.

机译：开发了一种有效的途径来合成Fmoc保护的二肽4，其含有α-亚甲基β-氨基酸的Gly-Gly的同等异构体;分别通过改变生物活性显着低于母体化合物的天然化合物3a和3b中的Gly〜2-Gly〜3的4来制备亮氨酸脑啡肽3a和蛋氨酸脑啡肽3b的构象化类似物。

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《Amino acids》 |2010年第4期|共9页
作者
Roberta Galeazzi; Gianluca Martelli; Eleonora Marcucci;
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原文格式 PDF
正文语种 eng
中图分类生物化学;
关键词
Isostere; Dipeptide; Conformational restriction; Baylis-Hillman; Activity;

机译：等位基因;二肽;构象限制;Baylis-Hillman;活动;

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1. Analogues of both Leu- and Met-enkephalin containing a constrained dipeptide isostere prepared from a Baylis-Hillman adduct [J] . Roberta Galeazzi, Gianluca Martelli, Eleonora Marcucci Amino acids . 2010,第4期

机译：由Baylis-Hillman加合物制备的含有受约束的二肽等排物的Leu-和Met-脑啡肽的类似物
2. An efficient synthetic method for Z-fluoroalkene dipeptide isosteres:Application to the synthesis of the dipeptide isostere of Sta-Ala [J] . Yuko Nakamura, Midori Okada, Minoru Koura, Journal of Fluorine Chemistry . 2006,第4a5期

机译：Z-氟烯烃二肽等位基因的有效合成方法：在Sta-Ala二肽等位基因的合成中的应用
3. Synthesis of a tricyclic delta-amino acid as a constrained Gly-Asn dipeptide isostere [J] . A.Ti-abocchi, G.Menchi, E.Danieli Amino acids . 2008,第1期

机译：限制Gly-Asn二肽等排体的三环δ-氨基酸的合成
4. Analogues of arginine vasopressin modified in position 2 and 3 with conformationally constrained dipeptide fragments [C] . Elzbieta Lempicka, Izabela Derdowska, Wioleta Kowalczyk International Peptide Symposium;European Peptide Symposium . 2005

机译：在第2和3位修饰的精氨酸血管素的类似物，具有构象约束的二肽片段
5. Total synthesis and biological evaluation of fluoroolefin-containing dipeptide isosteres as inhibitors of dipeptidyl peptidase IV (CD26). [D] . Lin, Jian. 1998

机译：作为二肽基肽酶IV（CD26）抑制剂的含氟烯烃的二肽等位基因的全合成和生物学评估。
6. Science letters: A convenient and stereoselective synthesis of (Z)-allyl selenides via Sm/TMSCl system-promoted coupling of Baylis-Hillman adducts with diselenides [O] . Yun-kui Liu, Dan-qian Xu, Zhen-yuan Xu, 2006

机译：科学字母：通过Sm / TMSCl系统促进的Baylis-Hillman加合物与二硒化物的偶联方便且立体选择性地合成（Z）-烯丙基硒化物
7. Synthesis of a bicyclic δ-amino acid as a constrained Gly-Asn dipeptide isostere [O] . A. Trabocchi, G. Menchi, E. Danieli, 2008

机译：双环δ-氨基酸的合成为约束的甘氨酸二肽等离子
8. DNA Adduct Formation by 7,12-Dimethylbenz(a)anthracene and its Noncarcinogenic 2-Fluoro Analogue in female Sprague-Dawley Rats [R] . Daniel, F. B. , Joyce, N. J. 1982

机译：7,12-二甲基苯（a）蒽及其非致癌2-氟类似物在雌性sprague-Dawley大鼠中形成DNa加合物

Analogues of both Leu- and Met-enkephalin containing a constrained dipeptide isostere prepared from a Baylis-Hillman adduct

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