Synthesis and in vitro evaluation of novel tetrazole embedded 1,3,5-trisubstituted pyrazoline derivatives as Entamoeba histolytica growth inhibitors
- Synthesis and in vitro evaluation of novel tetrazole embedded 1,3,5-trisubstituted pyrazoline derivatives as Entamoeba histolytica growth inhibitors
- 최인호; Mohmmad Youns Wani[Mohmmad Youns Wani]; 압둘루프바트; Amir Azam[Amir Azam]; 이대형; Fareeda Athar[Fareeda Athar]
- METRONIDAZOLE-INDUCED ENCEPHALOPATHY; ANTIMICROBIAL AGENTS; CELLS; GENOTOXICITY; CHEMISTRY; ASSAY
- Issue Date
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.54, pp.845 - 854
- A series of pyrazoline derivatives (1a-15a) was synthesized by cyclization of chalcones (1-15) with 2-[5-(4-methoxyphenyl)-1H-tetrazol-1-yl]acetohydrazide under basic conditions and were screened in vitro, to find out effect on the growth of HM1: IMSS strain of Entamoeba histolytica. The compounds 3a, 4a, 11a, 13a and 14a showed encouraging results with IC50 value in the range of 0.86-1.28 mu M. However compound 13a showed most promising results with IC50 = 0.86 mu M which is half of the metronidazole, the standard drug used for protozoal infection. Cell viability test in human hepatocellular carcinoma cell line (HepG2) revealed non-toxic nature of new synthesized compounds. Safety index calculations prevailed compound 13a as highly antiamoebic and least cytotoxic (S.I. = >116.28), almost twice than metronidazole. (C) 2012 Elsevier Masson SAS. All rights reserved.
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