Synthesis and in vitro biological evaluation of fluoro-substituted-4-phenyl-1,2,3,6-tetrahydropyridines as monoamine oxidase B substrates

被引：36

作者：

Beeler, AB

Sarma, R

Gadepalli, VS

Steyn, S

Castagnoli, N

Rimoldi, JM ^{[1
]}

机构：

[1] Univ Mississippi, Dept Med Chem, University, MS 38677 USA

[2] Univ Mississippi, Lab Appl Drug Design & Synth, University, MS 38677 USA

[3] Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 23期

关键词：

D O I：

10.1016/j.bmc.2003.08.002

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The substrate properties of three beta-fluoro-4-phenyl-1,2,3,6-tetrahydropyridines related to the proneurotoxin 1-methyl-4phenyl-1,2,3,6-tetrahydropyridine have been examined in an effort to evaluate the contribution of electronic parameters to the MAO-B catalyzed allylic-alpha-carbon oxidation of the tetrahydropyridinyl system. The design, synthesis, and biological evaluation of these analogues are presented and correlations to amine ionization potentials versus substrate activity are discussed. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：5229 / 5234

页数：6

共 36 条

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