Two series of 1-alkyl-4-(4H-1,2,4-triazol-4-yl)piperidines and 1-alkyl-4-(2H-1,2,4-triazol-3-one-4-yl) piperidines
were synthesized and their anticonvulsant and antibacterial activities were evaluated. Pharmacological tests showed
that three of the synthesized compounds (6c, 6k, 7m) displayed 100% protection at a dose of 100 mg/kg. 4-(1-
Octylpiperidin-4-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one (6c) was the most active compound in this study, with an ED50 of
65.4 mg/kg and a TD50 value of 241.2 mg/kg, resulting in a PI of 3.6. Four of the synthesized compounds showed potent
inhibitory activity against gram positive bacteria staphylococcus aureus (RN4220, KCTC 209 and KCTC 503), especially
against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compound
1-tetradeyl-4-(4H-1,2,4-triazol-4-yl)piperidine (7f) showed the most potent levels of activity (MIC = 2 µg/mL)
against the gram-positive strains.
Antibacterial, anticonvulsant, maximal electroshock test, synthesis, triazole, tiazolone.
Medicinal Chemistry and Pharmacology Institute, Inner Mongolia University for the Nationalities, No. 22 Huolin He Street, Tongliao City, Inner Mongolia, 028000, P.R. China