European Journal of Medicinal Chemistry p. 89 - 94 (2014)
Update date:2022-08-15
Topics:
Guo, Xiaoke
Ma, Xianglei
Yang, Qian
Xu, Jing
Huang, Lu
Jia, Jianmin
Shan, Jiaojiao
Liu, Li
Chen, Weilin
Chu, Hongxi
Wei, Jinlian
Zhang, Xiaojin
Sun, Haopeng
Tang, Yiqun
You, Qidong
Kv1.5 potassium channel is an efficacious and safe therapeutic target for the treatment of atrial fibrillation (AF), the most common arrhythmia that threatens human. Herein, by modifying the hit compound 7k from an in-house database, 48 derivatives were synthesized for the assay of their Kv1.5 inhibitory effects by whole cell patch clamp technique. Six compounds which showed better potency than the positive compound dronedarone were selected for the next evaluation of their drug-like properties. Compound 8 exhibited balanced solubility and permeability. It also showed acceptable pharmacodynamics profile with very low acute toxicity. Taking all these data into account, compound 8 can serve as a promising lead for the development of novel therapeutic agent for the treatment of AF.
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