1,2-Disubstituted bicyclo[2.1.1]hexanes as saturated bioisosteres of ortho-substituted benzene,Chemical Science

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1,2-Disubstituted bicyclo[2.1.1]hexanes as saturated bioisosteres of ortho-substituted benzene
Chemical Science ( IF 7.6 ) Pub Date : 2023-10-27 , DOI: 10.1039/d3sc05121h
Aleksandr Denisenko ₁ , Pavel Garbuz ₁ , Yelyzaveta Makovetska ₁ , Oleh Shablykin _{1,

2} , Dmytro Lesyk ₃ , Galeb Al-Maali _{1,

4} , Rodion Korzh ₁ , Iryna V Sadkova ₁ , Pavel K Mykhailiuk ₁

Affiliation

Bicyclo[2.1.1]hexanes have been synthesized, characterized, and biologically validated as saturated bioisosteres of the ortho-substituted benzene ring. The incorporation of the 1,2-disubstituted bicyclo[2.1.1]hexane core into the structure of fungicides boscalid (BASF), bixafen (Bayer CS), and fluxapyroxad (BASF) gave saturated patent-free analogs with high antifungal activity.

中文翻译：

1,2-二取代双环[2.1.1]己烷作为邻位取代苯的饱和生物等排体

双环[2.1.1]己烷已被合成、表征和生物学验证为邻位取代苯环的饱和生物等排体。将 1,2-二取代的双环[2.1.1]己烷核心纳入杀菌剂啶酰菌胺 (BASF)、bixafen (拜耳 CS) 和 Fluxapyroxad (BASF) 的结构中，得到具有高抗真菌活性的饱和无专利类似物。

更新日期：2023-10-27

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