title: Synthesis and in vitro biological evaluation of fluoro-substituted-4-phenyl-1,2,3,6-tetrahydropyridines as monoamine oxidase B substrates.
abstract: The substrate properties of three beta-fluoro-4-phenyl-1,2,3,6-tetrahydropyridines related to the proneurotoxin 1-methyl-4-phenyl-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.
authors: Department of Medicinal Chemistry and Laboratory for Applied Drug Design and Synthesis, University of Mississippi, University MS 38677, USA.
authors: Aaron B
authors: AB
authors: Beeler
authors: Rama Sarma V S
authors: RS
authors: Gadepalli
authors: Salome
authors: S
authors: Steyn
authors: Neal
authors: N
authors: Castagnoli
authors: John M
authors: JM
authors: Rimoldi
mesh_terms: D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D008995:Monoamine Oxidase / Q000378:metabolism*; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D013379:Substrate Specificity
chemical_list: D011725:Pyridines; D008995:Monoamine Oxidase