Journal of Medicinal Chemistry p. 117 - 121 (1988)
Update date:2022-07-31
Topics:
DeBernardis, J. F.
Gifford, P.
Rizk, M.
Ertel, R.
Abraham, D. J.
Siuda, J. F.
A number of quaternary salts of trans-4-(β-1-naphthylvinyl)pyridine (NVP) were synthesized and evaluated as inhibitors of the enzyme choline acetyltransferase (ChAT) and acetylcholinesterase (AChE).Structural variations in the side arm attashed to the pyridine nitrogen atom demonstrate that an inductive effect is small but significant for activity.Inhibition of ChAT by alkylated derivatives decreases when electron-withdrawing groups are placed in the side chain.Substitution of a methyl group on the pyridine ring only slightly affects activities toward ChAT and AChE.When the pyridinium moiety is replaced by an imidazolium ring, no ChAT inhibition was observed.The imidazolium compound, however, was a weak inhibitor of AChE.For design of affinity columns for purification of ChAT, the data also support the use of long chain alkylated amide derivatives of NVP.
View MoreNanjing Fayekong Chemcial Co.,Ltd(expird)
Contact:86-25-58813444
Address:Rm 1503, Unit 1, Building 5, Zijinnanyuan, Nanjing, Jiangsu, China
Anhui New Star Pharmaceutical Development Co., Ltd
Contact:013956922763
Address:Floor 3, F9A, F Workshop, No.110 Kexue Road, High-Tech Development Zone, Hefei, Anhui ,China
Wuhan Chemchemical Co., Ltd.(expird)
Contact:15973022782
Address:7-5-6218,Incubation Centre,Guandong Industry Park, East Lake High-Tech Development Zone,Wuhan City.
Baoding City Light Industry And Textiles Imp.& Exp. Corp. Chemical Department.
Contact:86-312-3262436
Address:NO.658 CHAOYANG SOUTH STREET,BAODING CITY HEBEI CHINA
website:http://www.antimex.com
Contact:0086-21-50563169
Address:Room1027,No.Jinyu Road,Pudong
Doi:10.1139/v84-055
(1984)Doi:10.1002/mrc.1270150103
(1981)Doi:10.1248/cpb.31.3503
(1983)Doi:10.1016/j.ica.2005.11.018
(2006)Doi:10.1248/cpb.c14-00329
(2014)Doi:10.1016/0022-328X(93)83287-6
(1993)