Journal of Medicinal Chemistry p. 3618 - 3625 (2017)
Update date:2022-08-23
Topics:
Zhang, Chen
Li, Fangqiong
Yu, Yan
Huang, Anbang
He, Ping
Lei, Ming
Wang, Jianmin
Huang, Longbin
Liu, Zhenhong
Liu, Jianyu
Wei, Yonggang
In the present work, a series of structurally novel benzocyclobutene derivatives were identified as general anesthetics through the loss of righting reflex (LORR) experiment on mice. Our initial efforts found compound 1a with a fused four-membered ring on the 2,3-position of the phenol ring could significantly improve the safety profile. Further SAR study revealed that small hydrogen bond acceptor (HBA) groups are optimal for good ED50 along with much broader therapeutic windows, such as compounds 16b and 17. Present work demonstrates the superiority of this novel benzocyclobutene scaffold.
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