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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.