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.
View MoreMS( MAOSHENG )Chemical CO.,LTD
Contact:+86-519-82726678.82726378
Address:TAOXI INDUSTRY ZONE JINTAN
Contact:+852-8198 2399
Address:9E, Leapont Industrial Building, 18-28 Wo Liu Hang Road, Shatin, New Territories, Hong Kong
Shandong Xiangde Biotechnology Co., Ltd
Contact:+86 -15066639877
Address:Sanba street
Contact:86-28-61993785
Address:No.70-13-21, North Section, Erhuan
Yancheng Creator Chemical Co., Ltd
Contact:0086-515-88710008 88710068 88710858 88710868
Address:No.21 Renming Road, Longgang Town, Yandu County,Yancheng City
Doi:10.1016/S0040-4020(01)93032-7
(1970)Doi:10.1016/j.tetlet.2013.02.046
(2013)Doi:10.1021/acs.joc.5b02251
(2015)Doi:10.3390/molecules18021963
(2013)Doi:10.1002/hc.21058
(2013)Doi:10.1021/acs.orglett.7b00793
(2017)