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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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