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.

MAOI ACTIVITY OF THIOSEMICARBAZIDES AND RELATED 2-THIAZOLYLHYDRAZINES

PIGNATELLO, Rosario;CASTELLI, Francesco;RACITI G;
1994-01-01

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/27836
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