Tripathi Purnima, Tripathi Avinash C, Chawla Viney, Saraf Shailendra K
Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India.
Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India.
Eur J Med Chem. 2014 Jul 23;82:439-48. doi: 10.1016/j.ejmech.2014.05.080. Epub 2014 Jun 2.
A novel series of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-one derivatives (1c-3c and 5c) were synthesized, via base catalyzed nucleophilic substitution of N-chloroacetyl-2,6-diarylpiperidin-4-ones (1b-6b) with N-methyl piperazine. The newly synthesized compounds were characterized by FTIR, Mass and NMR spectral studies. All the compounds were screened for their possible analgesic and antipyretic activities. The compound 2c exhibited promising antipyretic activity, comparable to that of paracetamol at 60 mg/kg dose. The compounds 2b and 2c showed significant analgesic profile at a dose of 60 mg/kg and were also found to be more potent than the reference drug, diclofenac sodium. Thus, it can be concluded that the synthesized 2,6-diarylpiperidin-4-ones exhibit promising antipyretic and analgesic activities and could be potential drug candidates.
通过N - 氯乙酰基 - 2,6 - 二芳基哌啶 - 4 - 酮（1b - 6b）与N - 甲基哌嗪的碱催化亲核取代反应，合成了一系列新型的N - （N - 甲基哌嗪基乙酰基） - 2,6 - 二芳基哌啶 - 4 - 酮衍生物（1c - 3c和5c）。通过傅里叶变换红外光谱（FTIR）、质谱和核磁共振光谱研究对新合成的化合物进行了表征。对所有化合物进行了潜在的镇痛和解热活性筛选。化合物2c表现出有前景的解热活性，在60mg/kg剂量下与对乙酰氨基酚相当。化合物2b和2c在60mg/kg剂量下显示出显著的镇痛效果，并且还发现其比参比药物双氯芬酸钠更有效。因此，可以得出结论，合成的2,6 - 二芳基哌啶 - 4 - 酮具有有前景的解热和镇痛活性，可能是潜在的药物候选物。
