380424-99-7Relevant academic research and scientific papers
Synthesis and studies on anticonvulsant and antibacterial activities of 1-Alkyl-4-(4H-1,2,4-triazol-4-yl)piperidine derivatives
Yuan, Yan-Ping,Wang, Shi-Ben,Gong, Guo-Hua,Quan, Zhe-Shan
, p. 1070 - 1078 (2015/04/14)
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 ug/mL) against the gram-positive strains.
The design and synthesis of purine inhibitors of CDK2. III
Shum,Peet,Weintraub,Le,Zhao,Barbone,Cashman,Tsay,Dwyer,Loos,Powers,Kropp,Wright,Bitonti,Dumont,Borcherding
, p. 1067 - 1078 (2007/10/03)
Cyclin-dependent kinases (CDKs) belong to a class of enzymes that control the ability of a cell to enter into and proceed through the cell division cycle. Using purine as a scaffold, we have synthesized a number of nanomolar inhibitors of CDK-2/cyclin E. In this report, the synthesis of a series of piperidine-substituted purine analogs will be presented, as well as some of their in vitro and in vivo biological effects.
