Bioorganic and Medicinal Chemistry Letters p. 475 - 480 (1999)
Update date:2022-08-04
Topics:
Britton, Thomas C.
Spinazze, Patrick G.
Hipskind, Philip A.
Zimmerman, Dennis M.
Zarrinmayeh, Hamideh
Schober, Douglas A.
Gehlert, Donald R.
Bruns, Robert F.
A series of benzo[b]thiophene-derived NPY-1 receptor antagonists is described. Systematic modification of the C-2 substituent afforded a 1000- fold range in Y1 receptor affinity. Appropriate substitution at the ortho and para positions of the C-2 phenyl ether produced a synergistic effect on Y1 binding affinity, which led to the discovery of the most active ligands, 12t (K(i) = 15 nM), 12u (K(i) = 11 nM), and 12v (K(i) = 13 nM).
View MoreQINGDAO TAOSIGN INTERNATIONAL TRADE CO.,LIMITED
Contact:+86-0532-82683616
Address:RM1402, Doublestar Seacoase 7#, No. 5 Guizhou Road, Qingdao, Shandong, China
shijiazhuang shuanglian chemical industry co.,ltd
Contact:0311-82190302
Address:Luquan Intersection , Shijiazhuang--Taiyuan Expressway,Shijiazhuang City
WuHan rongfashun BioChemical co., LTD
Contact:02788866139
Address:No.95 LuoYu Road,Wuhan
Contact:+86-27-87204219, +86-27-87215023
Address:2402, HuiGu Space-time Building, 8 Forest Road, East Lake Hi-Tech Development Zone
Tianjin Ingenochem Technology Co.,Ltd
Contact:+86-22-23677060
Address:Hitech Green Industry Park K2-9-602, Nankai district
Doi:10.1016/0040-4020(76)85179-4
(1976)Doi:10.1016/j.bioorg.2019.103480
(2020)Doi:10.1021/jacs.1c06906
(2021)Doi:10.1002/adsc.202000202
(2020)Doi:10.1021/ja982696q
(1998)Doi:10.1021/ja01238a035
(1944)