Synthesis, Antidepressant Activity, and Prediction of Toxic Risks of 3-Alkoxy(Sulfanyl)Thietane-1,1-Dioxides

Autor:	E. E. Klen, I. L. Nikitina, F. A. Khaliullin, N. N. Makarova, G. G. Gaisina
Rok vydání:	2020
Předmět:	Pharmacology Thietane 010405 organic chemistry medicine.drug_class Sodium Pharmacology toxicology chemistry.chemical_element 01 natural sciences Medicinal chemistry Anxiolytic 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Sulfanyl Drug Discovery Alkoxy group medicine Antidepressant Amitriptyline medicine.drug
Zdroj:	Pharmaceutical Chemistry Journal. 53:1106-1112
ISSN:	1573-9031 0091-150X
DOI:	10.1007/s11094-020-02131-z
Popis:	A series of 3-alkyloxy(sulfanyl)thietane-1,1-dioxides were synthesized by reacting 3,5-dibromo-1-(1,1-dioxothietanyl- 3)-1,2,4-triazole with sodium alkoxides and thioalkoxides. Compounds IIa (2 mg/kg) and IIh (6 mg/kg) exhibited antidepressant-like effects at doses equimolar to amitriptyline (10 mg/kg); IId (2 mg/kg) and IIb (2 and 5.7 mg/kg), effects associated presumably with anxiolytic properties. Prediction of toxic risks, drug-likeness, and physicochemical properties of the molecules using the Osiris DataWarrior and Property Explorer programs showed that the compounds should not have adverse effects on reproductive functions and should not possess oncogenic, mutagenic, and irritant properties.
Databáze:	OpenAIRE
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