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Updated: Jun 26, 2025

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

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Published on: September 28, 2022

通过Imidazopyridinium移植合成膜透的宏环

Bo Li¹, Joshua Parker¹, Joel Tong¹

¹Department of Chemistry, The Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology, 120 Scripps Way, Jupiter, Florida 33458, United States.

Journal of the American Chemical Society

|May 16, 2024

概括

通过一种新的imidazopyridinium (IP+) 连接合成了具有改善细胞透性的新型宏环 (MPs). 这一突破增强了MP作为具有挑战性的蛋白质标药物的潜力.

科学领域:

医学化学
有机合成
药物发现

背景情况:

宏环 (MPs) 对难以向的蛋白质有效,但细胞透性和生物可用性较差.
现有的限制阻碍了宏环的治疗应用.

研究的目的:

开发具有增强膜透性的新型宏环的高效合成方法.
探索一种新的化学策略来创造多样化的宏循环结构.

主要方法:

开发了一种固相合成方法,以创建与伊米达皮里迪尼 (IP+) 结合的宏循环.
使用可逆的分子内胺结合与胺衍生物.
各种尺寸和配置的合成宏循环 (头对侧,侧对侧).

主要成果:

实现了新型IP+相关的宏环的高效合成.
与传统分子相比,IP+连接的MP显著提高了被动膜透性.
已证实适用于图书馆合成和选蛋白质配体.

结论:

新的IP+链接宏循环化学克服了传统宏循环的关键限制.
这种方法为开发具有增强生物可用性的新疗法提供了有前途的策略.
合成的库对于识别新型蛋白质配体非常有价值.

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相关概念视频

Preparation of Amides

Preparation of Amides

Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...