Abstract
The preparation is described of hydrazides I, thiosemicarbazides II, III, IV and hydrazinothiazoles VIII, which can be considered as "precursors" or "open models" for the synthesized benzoyl-, benzilidene- and benzyl-hydrazinothiazoles V, VI and VII, analogous to 4-methyl and 4-phenyl substituted derivatives A, B and C, described and tested for their MAOI activity in a previous paper. Biochemical assay on the new prepared compounds allowed us to better clarify the structure-activity relationship also of compounds A, B and C of the precedent note. Moreover, on a group of derivatives, which showed a higher activity, a further test was performed to observe the possible correlation between MAOI activity and both their lipophilicity and ability in interacting with liposome bilayers, taken as a model of cell membrane.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Brain / enzymology
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Calorimetry, Differential Scanning
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Cell Membrane / metabolism
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Chemical Phenomena
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Chemistry, Physical
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Female
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Hydrazines / chemical synthesis*
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Hydrazines / chemistry
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Hydrazines / pharmacology
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In Vitro Techniques
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Lipids / chemistry
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Male
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Mitochondria / drug effects
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Mitochondria / enzymology
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Monoamine Oxidase Inhibitors / chemical synthesis*
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Monoamine Oxidase Inhibitors / chemistry
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Monoamine Oxidase Inhibitors / pharmacology
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Rats
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Spectrometry, Fluorescence
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology
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Thiosemicarbazones / chemical synthesis*
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Thiosemicarbazones / chemistry
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Thiosemicarbazones / pharmacology
Substances
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Hydrazines
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Lipids
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Monoamine Oxidase Inhibitors
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Thiazoles
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Thiosemicarbazones