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解锁新的前化模式:阿扎醇作为印烯基转移酶的新基质类

Eric D Gardner¹, Bryce P Johnson¹, Dustin A Dimas¹

¹Department of Chemistry and Biochemistry, University of Oklahoma, Stephenson Life Sciences Research Center, Norman, Oklahoma 73019, United States.

|November 13, 2023

概括

药物化学家探索了前转移酶 (PTs) 以功能化阿赞醇类似物. 这项研究扩大了获得新化学空间的机会,以发现新的生物活性化合物.

科学领域:

药用化学医学化学
酶学是一种酶学.
有机合成有机合成

背景情况:

阿扎替代增强了溶解度,但获得功能化的阿扎是具有挑战性的.
印度醇化芳香性前转移酶 (PTs) 是一种修改自然产品的酶.
开发新方法来合成功能化的阿赞多尔对于药物发现至关重要.

研究的目的:

探索使用醇化PT用于直接功能化阿扎醇类似物.
为了合成aza-l-tryptophans (Aza-Trp) 和循环Aza-Trp-proline (Aza-CyWP) dipeptides作为基质模仿剂.
根据替代模式,研究先化的区域选择性.

主要方法:

合成阿扎-l-三和阿扎-三-二类似物.
合成的类似物与特定的醇化PTs (FgaPT2,CdpNPT,FtmPT1) 的化.
对前化产品的分析和区域选择性的确定.

主要成果:

几种azaindole基质类似物被PT接受.
N-替代的位置显著影响了前化的区域选择性.
FgaPT2产生了新的阳离子N-prenylpyridinium产品,揭示了一个新的先化模式.

结论:

的醇生物异构体可以是PT的基质.
这项工作为indulediketopiperazine类似物提供了新的化学空间.
这些发现为药物化学和药物发现开辟了新的途径.

关键词:

生物催化剂是一种生物催化剂.化学选择性化学选择性酶催化酶的催化作用自然产品自然产品异环异环是一种异环.

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