Synthesis of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives and evaluation of their antidepressant and anxiolytic activity.
J Med Chem
; 44(6): 931-6, 2001 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-11300875
ABSTRACT
Recently a series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives bearing different substituents were synthesized and screened pharmacologically in order to evaluate their central nervous system activity. The purpose of this study was to evaluate the effects of the title compounds on CNS activity by varying the substituents in the thiadiazole moiety. It was found that some of these compounds possess marked antidepressant and anxiolytic properties comparable in efficiency to the reference drugs Imipramine and Diazepam. The most potent compound 3k was further investigated to complete its pharmacological profile with respect to undesired side effects. Behavioral results showed that 3k is a very promising compound, characterized by a mixed antidepressant-anxiolytic activity accompanied by a therapeutic dose range that is essentially 2 orders of magnitude less than that at which side effects such as sedation and amnesia are evident.
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Base de dados:
MEDLINE
Assunto principal:
Sulfetos
/
Tiadiazóis
/
Ansiolíticos
/
Antidepressivos
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article