Synthesis and in vitro evaluation of novel tetrazole embedded 1,3,5-trisubstituted pyrazoline derivatives as Entamoeba histolytica growth inhibitors

Title
Synthesis and in vitro evaluation of novel tetrazole embedded 1,3,5-trisubstituted pyrazoline derivatives as Entamoeba histolytica growth inhibitors
Author(s)
최인호Mohmmad Youns Wani[Mohmmad Youns Wani]압둘루프바트Amir Azam[Amir Azam]이대형Fareeda Athar[Fareeda Athar]
Keywords
METRONIDAZOLE-INDUCED ENCEPHALOPATHY; ANTIMICROBIAL AGENTS; CELLS; GENOTOXICITY; CHEMISTRY; ASSAY
Issue Date
201208
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.54, pp.845 - 854
Abstract
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.
URI
http://hdl.handle.net/YU.REPOSITORY/27573http://dx.doi.org/10.1016/j.ejmech.2012.03.049
ISSN
0223-5234
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생명공학부 > 생명공학부 > Articles
의과대학 > 산부인과학교실 > Articles
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