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功能化的2-thiobenzazole支架的DNA兼容的组合合成

Xianfeng Li¹, Changyang Liu¹, Yuting Gao¹

¹Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, China. yizhouli@cqu.edu.cn.

Chemical communications (Cambridge, England)

|July 13, 2023

概括

研究人员开发了一种新的DNA兼容的方法来合成2-thiobenzazole支架. 这种方法可以有效地在DNA上结合硫,扩大DNA编码的化学库,用于药物发现.

科学领域:

药用化学医学化学
合成化学合成化学
化学生物学化学生物学

背景情况:

2 - 本醇是药物化学中的一个关键的异环基架.
DNA编码图书馆 (DEL) 为发现生物活性分子提供了一种高通量方法.
将特权支架集成到DEL中可以加速击中发现.

研究的目的:

开发一种DNA兼容的合成方法,用于构建功能化的2-thiobenzazole支架.
为了使图书馆扩张能够有效地在DNA上进行硫合并.
为了提高2-thiobenzazole聚焦的DELs的实用性.

主要方法:

为了合成2-thiobenzazole,使用了一种新的,温和的合成策略.
该方法是针对DNA兼容性进行了优化.
硫基组的结合直接在DNA上实现.

主要成果:

证明了功能化的2-thiobenzazole支架的高效合成.
该方法显示了硫烯合并的广泛基质范围.
成功的DNA合成扩大了基于2-thiobenzazole的DELs的多样性.

结论:

开发的方法为DELs中的2-thiobenzazole衍生物提供了一个简单的途径.
这种进步扩大了通过DEL技术可访问的化学空间.
这些发现有助于发现使用2-thiobenzazole支架的新生物活性化合物.

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