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对pH,氧化和小分子调节器反应的以胺酸盐为基础的循环

Anupam Bandyopadhyay¹, Jianmin Gao¹

¹Department of Chemistry, Merkert Chemistry Center, Boston College , 2609 Beacon Street, Chestnut Hill, Massachusetts 02467, United States.

Journal of the American Chemical Society

|February 10, 2016

概括

化学家开发了一种使用伊米诺酸盐的新循环法. 这种技术允许在生理条件下自发形成循环,并且可逆,在化学生物学中提供了多方面的应用.

科学领域:

化学生物学
有机化学
医学化学

背景情况:

类天然产品通常具有循环支架,以增强结的亲和力.
合成循环作为生物探测器和潜在治疗药物具有价值.
开发高效和多功能循环化策略仍然是一个关键挑战.

研究的目的:

引入一种新的循环化策略.
通过这种方法证明单环和双环的形成.
突出刺激反应和循环的可逆性.

主要方法:

为自发循环形成的分子内氨基酸.
使用生理条件进行循环.
调查因pH,氧化和小分子反应而产生的以伊米诺酸为基础的循环的可逆性.

主要成果:

通过 iminoboronate 的形成成功合成单环和双环.
在生理条件下自发循环的证明.
通过pH,氧化和小分子引发的快速和可逆循环的确认.

结论:

开发了一种基于伊米诺酸的新多功能循环化策略.
这种方法可以在生理条件下自发形成循环.
这种循环的刺激反应和可逆性为化学生物学和药物发现开辟了新的途径.

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