<p>[(1-Alkyl-3-methyl-2,6-dioxo-2,3,6,7-tetrahydro-1<i>H</i>-purin-8-yl)sulfanyl]acetic acids containing a thietane ring and their ethyl esters and hydrazides were synthesized based on 7-(thietan-3-yl)-, 7-(1-oxothietan-3-yl)-, and 7-(1,1-dioxothietan-3-yl)-1-alkyl-8-bromo-3-methyl-3,7-dihydro-1<i>H</i>-purine-2,6-diones. Most of the synthesized compounds exhibited antidepressant activity, influencing the duration of immobilization and the depression index in the tail-suspension test and the forced-swimming test. The strength of the antidepressant activity of the synthesized compounds did not statistically significantly differ from that of fluoxetine.</p>

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Synthesis and Antidepressant Activity of [(1-Alkyl-3-Methyl-2,6-Dioxo-2,3,6,7-Tetrahydro-1H-Purin-8-YL)Sulfanyl]Acetic Acids Containing a Thietane Ring

  • F. A. Khaliullin,
  • I. L. Nikitina,
  • Yu. V. Shabalina,
  • A. F. Miftakhova,
  • E. E. Klen,
  • R. A. Gubaeva,
  • A. V. Samorodov,
  • V. N. Pavlov

摘要

[(1-Alkyl-3-methyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)sulfanyl]acetic acids containing a thietane ring and their ethyl esters and hydrazides were synthesized based on 7-(thietan-3-yl)-, 7-(1-oxothietan-3-yl)-, and 7-(1,1-dioxothietan-3-yl)-1-alkyl-8-bromo-3-methyl-3,7-dihydro-1H-purine-2,6-diones. Most of the synthesized compounds exhibited antidepressant activity, influencing the duration of immobilization and the depression index in the tail-suspension test and the forced-swimming test. The strength of the antidepressant activity of the synthesized compounds did not statistically significantly differ from that of fluoxetine.