Synthesis and Studies on Anticonvulsant and Antibacterial Activities of 1- Alkyl-4-(4H-1,2,4-triazol-4-yl)piperidine Derivatives
Yan-Ping Yuan, Shi-Ben Wang, Guo-Hua Gong and Zhe-Shan Quan
Affiliation: Medicinal Chemistry and Pharmacology Institute, Inner Mongolia University for the Nationalities, No. 22 Huolin He Street, Tongliao City, Inner Mongolia, 028000, P.R. China
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.
Keywords: Antibacterial, anticonvulsant, maximal electroshock test, synthesis, triazole, tiazolone.
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