Inhibition des monoamine oxydases A et B par des dérivés d'aryl-2 4H-oxadiazine-1,3,4 (6H) ones-5

Three novel series of benzo[b]thiophene derivatives bearing various hydrazone, hydrazine and 1,3,4-oxadiazole moieties were synthesized as potential antidepressant agents. 22 Compounds were evaluated for their in vitro inhibitory effect on monoamine oxidase enzyme (MAO) type A. Several compounds inhibited MAO stronger than pargyline hydrochloride. Maximum inhibitions of 83% and 90% were observed with 1-benzyl-2-(3-chlorobenzo[b]thienyl-2-carbonyl)hydrazine (24) and 1-[2-(4-chlorophenyl)ethyl]-2-(3-chlorobenzo[b]thienyl-2- carbonyl)hydrazine (35), respectively.

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Novel Benzo[b]thienylhydrazine and 1,3,4‐Oxadiazole Derivatives as Potential Antidepressant Agents

Aboulwafa

El-Metwalli

1992

Archiv der Pharmazie

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ChemInform Abstract: Inhibition of Monoamine Oxidase Types A and B by 2‐Aryl‐4H‐1,3,4‐oxadiazin‐5(6H)‐one Derivatives.

et al. 1989

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ChemInform Abstract Monoamine oxidase (MAO) is responsible for the metabolic inactivation of amine neurotransmitters such as serotonin and dopamine. The title compounds of type (III) and (VI) are tested in vitro for their inhibitory effects on MAO A and MAO B. (IIIa) and (IIIb) with hydrophobic and electron-withdrawing R1 substituent, resp., inhibit MAO B, while (IIIc) are more active on MAO A. Replacement of the (CH2)2-CN moiety in (III) by the substituent R2 leads to the less active derivatives (VI). Introduction of a 6-methyl group into (Ib) decreases the inhibitor potency on MAO B.

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Synthesis and Monoamine Oxidase Inhibitory Activity of 3‐Substituted 5H‐Indeno[1,2‐c]pyridazines

Kneubühler

Testa

Carta

et al. 1993

Helvetica Chimica Acta

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Inhibition des monoamine oxydases A et B par des dérivés d'aryl-2 4H-oxadiazine-1,3,4 (6H) ones-5

Cited by 30 publications

References 21 publications

Novel Benzo[b]thienylhydrazine and 1,3,4‐Oxadiazole Derivatives as Potential Antidepressant Agents

Novel Benzo[b]thienylhydrazine and 1,3,4‐Oxadiazole Derivatives as Potential Antidepressant Agents

ChemInform Abstract: Inhibition of Monoamine Oxidase Types A and B by 2‐Aryl‐4H‐1,3,4‐oxadiazin‐5(6H)‐one Derivatives.

Synthesis and Monoamine Oxidase Inhibitory Activity of 3‐Substituted 5H‐Indeno[1,2‐c]pyridazines

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