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Published on: June 23, 2019
Synthesis and Biological Evaluation of 4-Aminoantipyrine Analogues
Houwei Ren1, Premnath Dhanaraj2, Israel V M V Enoch3
1Department of Emergency, Taizhou People's Hospital, Taizhou, Jiangsu, 225300,China.
Objectives:
The aim of the present study is to carry out a simple synthesis of aminoantipyrine analogues and exploration of their antibacterial, cytotoxic, and anticonvulsant potential.
Methods:
The compounds were characterized employing multi-spectroscopic methods. The in vitro pharmacological response of a series of bacteria was screened employing serial dilution method. The derivatives were screened against maximal electro-shock for their anticonvulsant activity. Molecular docking was carried out to optimize the interaction of the compounds with HPV16-E7 receptors. Further, the in vitro cytotoxicity was tested against human cervical cancer (SiHa) cell lines.
Results:
The compounds show protection against maximal electroshock, esp. 3-nirto- and 4- methyl-3-nitrobenzamido derivatives. In addition, they reveal appreciable DNA cleavage activities and interactions with HPV16-E7 protein receptors, esp. 3,5-dinitro- and 4-methyl-3-nitrobenzamido derivatives. Furthermore, they show potent activity against cervical cancer cells (LD50 value up to 1200 in the case of 4-methyl-3-nitrobenzamido derivative and an inhibition of a maximum of ~97% of cells).
Conclusion:
The simply synthesized aminoantipyrine derivatives show a variety of biological activities like antibacterial and anticancer effects. In addition, this is the first study demonstrating that 4-aminoantipyrine derivatives show an anticonvulsant activity.
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