Synthesis and analgesic activity of some acetamide derivatives


KAPLANCIKLI Z. A., ALTINTOP M. D., Turan-Zitouni G., ÖZDEMİR A., CAN Ö. D.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.27, no.2, pp.275-280, 2012 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 27 Issue: 2
  • Publication Date: 2012
  • Doi Number: 10.3109/14756366.2011.587417
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.275-280
  • Keywords: Acetamide, benzothiazole, tetrazole, hot-plate, writhing test, analgesic activity, CENTRAL-NERVOUS-SYSTEM, ANTINOCICEPTIVE ACTIVITY, MICE, INHIBITORS, PAIN
  • Bilecik Şeyh Edebali University Affiliated: No

Abstract

In the present study, some acetamide derivatives were synthesized and their potential analgesic activities were investigated. N-(benzothiazol-2-yl)-2-[(1-substituted-1H-tetrazol-5-yl) thio] acetamide derivatives were obtained by the nucleophilic substitution reaction of 2-chloro-N-(benzothiazole-2-yl) acetamides with appropriate tetrazol-5-thioles. The chemical structures of the compounds were elucidated by IR, H-1-NMR, C-13-NMR and FAB(+)-MS spectral data and elemental analyses. The prepared compounds were investigated for their potential analgesic properties against thermal, mechanical and chemical nociceptive stimuli using hot-plate, tail-clip and acetic acid-induced writhing tests, respectively. The assessment of motor coordination was carried out using Rota-Rod test. Tested compounds applied at 100 mg/kg doses caused significant decrease in acetic acid-induced writhing responses and increase in hot-plate and tail-clip latencies. None of the compounds exhibited destructive effect on motor coordination of the mice in Rota-Rod performance.