Browsing by Author "Erciyas, E"

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    Synthesis and antileishmanial activity of novel pyridinium-hydrazone derivatives
    Alptuzun, V; Cakiroglu, G; Limoncu, ME; Erac, B; Hosgor-Limoncu, M; Erciyas, E
    A series of substituted phenylethylidenehydrazinylpyridinium derivatives bearing methyl, ethyl, propyl, and propylphenyl groups on the pyridinium nitrogen were synthesized and evaluated for in vitro antileishmanial activity against Leishmania tropica by using the microdilution method. Among the tested compounds, 3d, 5c, 3b, and 3c were found to be the most active derivatives against the promastigotes of L. tropica (IC50 values are 6.90, 9.92, 11.69 and 12.03 mu M, respectively) and to be more active than reference drug meglumine antimonaite (glucantime) (IC50 value: 20.49 mu M). The derivatives investigated in this study may have the potential to be lead compound against leishmanial infection.
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    Design, synthesis, and in vitro biological evaluation of novel thiazolopyrimidine derivatives as antileishmanial compounds
    Istanbullu, H; Bayraktar, G; Akbaba, H; Cavus, I; Coban, G; Butuner, BD; Kilimcioglu, AA; Ozbilgin, A; Alptuzun, V; Erciyas, E
    A series of thiazolopyrimidine derivatives was designed and synthesized as aLeishmania majorpteridine reductase 1 (LmPTR1) enzyme inhibitor. TheirLmPTR1 inhibitor activities were evaluated using the enzyme produced byEscherichia coliin a recombinant way. The antileishmanial activity of the selected compounds was tested in vitro againstLeishmaniasp. Additionally, the compounds were evaluated for cytotoxic activity against the murine macrophage cell line RAW 264.7. According to the results, four compounds displayed not only a potent in vitro antileishmanial activity against promastigote forms but also low cytotoxicity. Among them, compoundL16exhibited an antileishmanial activity for both the promastigote and amastigote forms ofL. tropica, with IC(50)values of 7.5 and 2.69 mu M, respectively. In addition, molecular docking studies and molecular dynamics simulations were also carried out in this study. In light of these findings, the compounds provide a new potential scaffold for antileishmanial drug discovery.