The thiadiazole derivatives are known to possess several biological activities.¹ Therefore, thiadiazoles have been synthesized in our laboratory for a long time and their anticonvulsant, antidepressant, analgesic, and antimicrobial potentials have been investigated. Here, we would like to report preliminary evaluation of pharmacological and antimicrobial properties of six thiadiazoles with izoquinoline, indole, or thiadiazole ring at C-5 carbon atom.

Preliminary behavioral study showed that none of the tested compounds was found to show neurotoxic activity because in the dose of 0.1 LD₅₀ they did not affect the motor coordination of mice in the “chimney test”. All thiadiazole showed depressive activity in mice; they significantly prolonged the thiopental sleeping time in the “thiopental-induced sleep” test. Additionally, some compounds showed strong analgesic activity in the “writhing syndrome” test. Two compounds, which were tested as potential antimicrobials were inactive.

References

[1] (a) Farmaco 45 (1990) 134-139, (b) Bioorganic & Medicinal Chemistry Letters 14 (2004) 4615-4621, (c) European Journal of Medicinal Chemistry 44 (2009) 1250-1256, (d) Bioorganic & Medicinal Chemistry 13 (2005) 5330-5337, (e) Bioorganic & Medicinal Chemistry 11 (2003) 185-192, (f) Bioorganic & Medicinal Chemistry 18 (2010) 590-596, (g) European Journal of Medicinal Chemistry 44 (2009) 2828-2833, (h) European Journal of Medicinal Chemistry 43 (2008) 808-815, (i) European Journal of Medicinal Chemistry 44 (2009) 2313-2321.

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