The cyclization reaction of 4-substituted 1-[(piperidin-4-yl)-carbonyl]thiosemicarbazides 1 gave 4-substituted 3-(piperidin-4-yl)-Δ²-1,2,4-triazoline-5-thiones 2.

Cyclic compounds 2 with R = C₆H₅, 4-BrC₆H₅, 4-I-C₆H₅ were screened for their antimicrobial activity in vitro against 14 species of aerobic bacteria and 12 species of fungi. MIC (Minimal Inhibitory Concentration) values defined as the lowest concentration of compounds required to inhibit the visible growth of the tested microorganism, was estimated by agar-dilution method. Petri dishes containing Mueller-Hinton agar (for bacteria) or RPMI 1640 agar (for fungi) and the compounds at a concentration of 31.25-500 mg/mL were inoculated with a culture size no. 0.5 McFarland Standards and incubated at 37 ^oC for 18 h for bacteria and at 30 ^oC for 5 days for fungi. The growth of microorganisms were compared with a control culture without the tested compounds. The compounds 2 with R = C₆H₅ and R = 4-I-C₆H₅ were not active against bacteria, however, compound 2 with R = 4-BrC₆H₅ partially inhibited the growth of Staphylococcus sp. species (by about 80-95%) with values ranging from 125-500 mg/mL. All compounds were active against Trichophyton sp. with MIC values of 62.5-500 mg/mL, depending on the species. The tested compounds had not activity against yeast-like fungi and moulds. Only compound 2, R = 4-BrC₆H₅ affected the growth of Aspergillus niger with MIC value of 62.5 mg/mL.

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