Bioorganic and Medicinal Chemistry Letters p. 2263 - 2268 (1998)
Update date:2022-08-03
Topics:
Aslanian, Robert
Brown, Joan E.
Shih
Wa Mutahi, Mwangi
Green, Michael J.
She, Susan
Del Prado, Maurice
West, Robert
Hey, John
A series of amidine substituted phenyl-, benzyl-, and phenethylimidazoles based on the known H3 against SKandF 91606 (4) has been synthesized and tested as ligands for the histamine H3 receptor. Insertion of a phenyl ring between the imidazole ring and the amidine moiety produces antagonists. The benzyl series was found to be the most potent and was further investigated. Compounds 9c and 18 (entries 5 and 12, Table 1) are potent ligands for the H3 receptor with K(i) values of 16 nM and 7.2 nM respectively. In vivo, both compounds were shown to be equipotent to thioperamide (2), the standard H3 antagonist.
View MoreJinan Yijialian Economic and Trade Development Co., Ltd.
Contact:+86 0531-66729596
Address:jinan
website:http://www.np-chem.com
Contact:0086-25-52346877
Address:199, Jian Ye Road, Nanjing, China
Yingkou Sanzheng New Technology Chemical Industry Co., Ltd.
Contact:+86-417-2927806
Address:yingkou
Contact:
Address:
Hangzhou Gangjin Chemical Co.,Ltd.
Contact:+86-571-85109780
Address:707 Zhejiang Minhang Bldg., No.290 Zhongshan North Road, Hangzhou 310003, China
Doi:10.1021/ol801179x
(2008)Doi:10.1002/cctc.201200732
(2013)Doi:10.1021/ja00138a028
(1995)Doi:10.1002/chem.19970031123
(1997)Doi:10.1021/ja00081a058
(1994)Doi:10.1080/00397919508015850
(1995)