Ahad Faiza, Ghouri Nida, Khan Khalid Mohammed, Perveen Shahnaz, Choudhary M Iqbal
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
R Soc Open Sci. 2018 May 16;5(5):171771. doi: 10.1098/rsos.171771. eCollection 2018 May.
Leishmaniasis is a vector-borne protozoan disease; it mainly originates from the bite of sandfly and initiated when parasite is transmitted to human at metacyclic flagellated promastigote form. In the current study, a synthesis of a series of 4-substituted benzophenone ethers was carried out in good yields and their antileishmanial activities were also screened. Among synthetic derivatives, 15 compounds , , , and - showed antileishmanial activities against promastigotes of with IC values in the range of 1.19-82.30 µg ml, and the values were compared with those of the standard pentamidine (IC= 5.09 ± 0.09 µg ml). Our study identified a series of new antileishmanial molecules as potential leads. Structures of these synthetic compounds were deduced by different spectroscopic techniques, such as H and C nuclear magnetic resonance, electron impact and high-resolution electron impact mass spectrometry and IR.
利什曼病是一种媒介传播的原生动物疾病；它主要源于白蛉叮咬，当寄生虫以循环后期鞭毛前鞭毛体形式传播给人类时发病。在本研究中，一系列4-取代二苯甲酮醚以良好的产率合成出来，并对它们的抗利什曼活性进行了筛选。在合成衍生物中，15种化合物，，，和-对杜氏利什曼原虫前鞭毛体表现出抗利什曼活性，IC值在1.19 - 82.30μg/ml范围内，这些值与标准药物喷他脒（IC = 5.09±0.09μg/ml）的值进行了比较。我们的研究确定了一系列新的抗利什曼分子作为潜在的先导化合物。这些合成化合物的结构通过不同的光谱技术推导得出，如氢和碳核磁共振、电子轰击和高分辨率电子轰击质谱以及红外光谱。
