1,2-二取代双环[2.1.1]己烷作为α-取代苯的饱和生物电子等排体。
1,2-Disubstituted bicyclo[2.1.1]hexanes as saturated bioisosteres of -substituted benzene.
作者信息
Denisenko Aleksandr, Garbuz Pavel, Makovetska Yelyzaveta, Shablykin Oleh, Lesyk Dmytro, Al-Maali Galeb, Korzh Rodion, Sadkova Iryna V, Mykhailiuk Pavel K
机构信息
Enamine Ltd Winston Churchill st. 78 02094 Kyiv Ukraine www.mykhailiukchem.org
V. P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine 02094 Kyiv Ukraine.
出版信息
Chem Sci. 2023 Oct 27;14(48):14092-14099. doi: 10.1039/d3sc05121h. eCollection 2023 Dec 13.
Bicyclo[2.1.1]hexanes have been synthesized, characterized, and biologically validated as saturated bioisosteres of the -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.
双环[2.1.1]己烷已被合成、表征，并作为α-取代苯环的饱和生物电子等排体进行了生物学验证。将1,2-二取代双环[2.1.1]己烷核心引入杀菌剂啶酰菌胺（巴斯夫）、联苯吡菌胺（拜耳作物科学）和氟唑菌酰胺（巴斯夫）的结构中，得到了具有高抗真菌活性的无专利饱和类似物。
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