Positional isomers and analogs of mazindol as potential inhibitors of the cocaine binding site on the dopamine transporter site

被引：0
|
作者：
Houlihan, WJ
Boja, JW
Kopajtic, TA
Kuhar, MJ
Degrado, SJ
Toledo, L
机构：
[1] Drew Univ, Charles A Dana Res Inst, Madison, NJ 07940 USA
[2] NIDA, Addict Res Ctr, Baltimore, MD 21224 USA
来源：
MEDICINAL CHEMISTRY RESEARCH | 1998年 / 8卷 / 1-2期
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D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of compounds, where the keto-tautomeric form of mazindol (2b) was modified by placing the 2-(p-chlorobenzoyl) portion of the molecule in the 3- and 4-positions, substituting the imidazo ring A by a 4,4-dimethyl 1-2-oxazolo ring, and replacing the carbonyl group by a CHOH, CH2, O, S, SO and SO2 were prepared and evaluated for their ability to displace [H-3] WIN 35,428 binding in rat striatal tissue. All compounds were weaker (24-2,050-fold) than mazindol.
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页码：77 / 90
页数：14
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