Bioorganic and Medicinal Chemistry Letters p. 791 - 796 (2019)
Update date:2022-08-04
Topics:
Sharma, Swagat
Kozek, Krystian A.
Abney, Kristopher K.
Kumar, Sushil
Gautam, Nagsen
Alnouti, Yazen
David Weaver
Hopkins, Corey R.
The present study describes the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-ylacetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, we identified a tetrazole scaffold that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, we evaluated the compounds in Tier 1 DMPK assays and have identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups.
View MoreHangzhou Gangjin Chemical Co.,Ltd.(expird)
Contact:+86-571-85109780
Address:707 Zhejiang Minhang Bldg., No.290 Zhongshan North Road, Hangzhou 310003, China
website:http://www.amadischem.com
Contact:86-571-89925085
Address:Watts Cosine.No.166.Xiangmao Road.
Jewim Pharmaceutical (Shandong) Co., Ltd
Contact:+8615621883869
Address:山东省泰安市高新技术产业开发区配天门大街西首
SHIFANG SUHONG CHEMICAL CO.,LTD
Contact:+86-838-2224563
Address:Room 1207 Zongchen Sunshine No.128 Taishan South Road,Deyang City,Sichuan China
SICHUAN ZHONGBANG NEW MATERIAL CO., LTD
website:http://www.zhongbangst.com
Contact:86-830-2585019
Address:sichuan,china
Doi:10.1016/S0040-4020(01)96748-1
(1985)Doi:10.1016/0008-6215(82)84032-9
(1982)Doi:10.1002/jhet.5570190423
(1982)Doi:10.1007/BF00503179
(1982)Doi:10.1021/ol402612x
(2013)Doi:10.1021/ic049765o
(2005)