Synthesis and in vitro evaluation of novel tetrazole embedded 1,3,5-trisubstituted pyrazoline derivatives as Entamoeba histolytica growth inhibitors.
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 IC(50) value in the range of 0.86-1.28 μM. However compound 13a showed most promising results with IC(50) = 0.86 μM 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.
Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, Maulana Ali Jauhar Marg, New Delhi-110025, India.
Mohmmad Younus
MY
Wani
Abdul Roouf
AR
Bhat
Amir
A
Azam
Dae Hyung
DH
Lee
Inho
I
Choi
Fareeda
F
Athar
D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D004748:Entamoeba histolytica / Q000187:drug effects* / Q000254:growth & development*; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013777:Tetrazoles / Q000737:chemistry*
D000981:Antiprotozoal Agents; D011720:Pyrazoles; D013777:Tetrazoles