Bioorganic and Medicinal Chemistry Letters (2020)
Update date:2022-08-04
Topics:
Temple, Kayla J.
Engers, Julie L.
Long, Madeline F.
Watson, Katherine J.
Chang, Sichen
Luscombe, Vincent B.
Jenkins, Matthew T.
Rodriguez, Alice L.
Niswender, Colleen M.
Bridges, Thomas M.
Conn, P. Jeffrey
Engers, Darren W.
Lindsley, Craig W.
This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, we investigated a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration.
View MoreShanghai Norky Pharmaceutical Co., LTD.
website:http://www.norkypharm.com
Contact:86-21-61075300
Address:1165 Jiangning Road, Office 1502, Shanghai, China
Contact:+86-28-88523492
Address:714rooms of Time Square, Pujiang County
WUXI HONOR SHINE CHEMICAL CO.,LTD
Contact:+86-510-83593312
Address:No.1699 Huishan avenue,Huishan district,Wuxi ,Jiangsu,China,214177.(Wuxi Huishan Ecomonic Develop Zone )
Hangzhou Yanshan Chemical Co.,Ltd.
Contact:86-571- 87698076
Address:Room 1001, #1 Building, Zhongtian MCC, No.2 Youzhinong, Wenyi West Road, Xihu District, Hangzhou, China
Tengzhou Runlong Fragrance Co., Ltd.
website:http://www.tzrunlong.com/
Contact:0086-15665710862
Address:No. 78, Fushan Road, Biomedical Industrial Park, Dawu Town, Tengzhou, Shandong, 277514 China
Doi:10.1016/S0040-4039(01)80210-0
(1984)Doi:10.1016/j.tet.2006.07.101
(2006)Doi:10.1070/MC2006v016n01ABEH002082
(2006)Doi:10.1039/c5ra00759c
(2015)Doi:10.1002/ejoc.201900356
(2020)Doi:10.1039/jr9630001858
(1963)