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Acta tropica v.167, 2017년, pp.73 - 78   SCI SCIE
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In vitro antileishmanial activity of novel azoles (3-imidazolylflavanones) against promastigote and amastigote stages of Leishmania major

Shokri, Azar (Student Research Committee, Department of Parasitology and Mycology, School of Medicine, Mazandaran University of Medical Sciences, Sari, Iran ) ; Emami, Saeed (Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran ) ; Fakhar, Mahdi (Molecular and Cell Biology Research Center, Department of Parasitology and Mycology, School of Medicine, Mazandaran University of Medical Sciences, Sari, Iran ) ; Teshnizi, Saeed Hosseini (Clinical Research Development Center of Children Hospital, Hormozgan University of Medical Sciences, Bandar Abbas, Iran ) ; Keighobadi, Masoud (Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran ) ;
  • 초록  

    Abstract Leishmaniasis is a protozoan infectious disease widely distributed all around the world. First line drugs including antimoniales are insufficient due to resistance in endemic areas and high toxicity. Azole antifungals like ketoconazole (KCZ) are also used as antileishmanial agents for several decades. In the present study, we evaluated in vitro antileishmanial effects of new azole antifungals namely 3-imidazolylflavanones (IFs) and their oximes (IFOs) against Leishmania major (L. major) parasites. The obtained results showed remarkable effect of our compounds on promastigote and amastigote stages of L. major . In particular, the 4-chloro analog of flavanone (IF-2) and 3-chloro substituted flavanone oxime (IFO-3) with IC 50 values ≤8.9μg/mL were 8-fold more potent than KCZ (IC 50 =7 72μg/mL) against promastigote form of L. major . In amastigote stage, the compounds IF-2 and IFO-2 decreased the mean number of infected macrophages (MIR) more than KCZ (p 50 value (115.4μg/mL) and SI (383.3). We concluded that our new synthetic azoles displaying potent activity against L. major could be considered as new hits for drug development in the field of antileishmanial therapy. Highlights In vitro anti-leishmanial activity of new synthesized azoles on promastigote and amastigotes of Leishmania major was evaluated. In vitro cytotoxicity of new synthesized azoles on J774 A.1 macrophage cells was evaluated. Reliable anti-leishmanial activity in decreasing both infected macrophages percentage and amastigotes was achieved. Prototype compound IF-2 showed better profile of activity respect to the standard azole ketoconazole. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Antileishmanial agents .   Azole antifungals .   Leishmania major .   Promastigote .   Amastigote .   Flavanones.  

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