由于利什曼病的化疗选择有限,新的合成化合物正在引起人们对利什曼病评估的关注。本研究旨在合成香兰素的席夫碱,以研究和评估其对细胞内原生动物寄生虫利什曼原虫的抗利什曼原虫的潜力。在目前的研究中,通过设计席夫碱与香兰素的协同作用现象增强了它们的期望重要性。使用不同的芳香胺和香兰素,总共合成了五个香兰素的席夫碱。通过FT-IR(傅里叶变换-红外)对所有化合物进行结构分析,薄层色谱,和光谱技术,如13C-NMR,质谱,和1H-NMR。在三种不同浓度25、50和100μg/ml下,分析了所有化合物ZI-1,ZI-2,BS-1,KH-1和FA-2对热带乳杆菌的前鞭毛虫和amastigotes形式的抗菌性能。进行体外MTT测定以计算抑制百分比,IC50值,和它们的细胞毒性。在25µg/ml时,对热带乳杆菌前鞭毛形式的最高抑制百分比值为BS-153.78%,ZI-2在50µg/ml时为66.95%,ZI-2在100微克/毫升时为76.92%。同样,在25μg/ml时,对细胞内amastigote阶段的最高抑制百分比值为BS-155.77%,ZI-2在50µg/ml时为67.78%,ZI-2为84.93%100µg/ml。在两个阶段中,BS-1的效力最高。针对前鞭毛体和细胞内阿马斯泰格体的IC50值为9.83和4.27µg/ml,分别。溶血百分比作为毒性;在三个不同的浓度分别为25、50、100µg/ml,分别为2.60、3.50和6.31时,ZI-1的溶血百分比最低。这些结果表明,所有化合物都表现出抗利什曼虫活性,BS-1是最有效的。进一步的研究建议通过添加一些其他协同作用来增加具有结构修饰的化合物的活性,小说,和类似物化合物。
Due to limited chemotherapeutic options for leishmaniasis, novel synthetic compounds are gaining attention for evaluation against leishmaniasis. This study aimed to synthesize the compound\'s Schiff bases of Vanillin to investigate and evaluate their anti-leishmanial potentials against intracellular protozoan parasites Leishmania tropica. In the current study, the phenomena of synergism by designing Schiff bases with Vanillin enhances their desired importance. A total of five compounds Schiff bases of Vanillin were synthesized using different aromatic amines and Vanillin. The structural analysis of all the compounds was done through FT-IR (Fourier Transformer-Infrared), thin layer chromatography, and spectroscopic techniques such as 13C-NMR, mass spectrometry, and 1H-NMR. The antimicrobial properties of all the compounds ZI-1, ZI-2, BS-1, KH-1, and FA-2 against
promastigotes and amastigotes forms of L. tropica were analyzed at three different concentrations 25, 50, and 100 µg/ml. The in-vitro MTT assay was performed to calculate the percent inhibition, IC50 values, and their cytotoxicity. The highest percent inhibition values against promastigote form of L. tropica were BS-1 53.78% at 25 µg/ml, ZI-2 66.95% at 50 µg/ml, and again ZI-2 76.92% at 100 µg/ml. Similarly, the highest percent inhibition values against intracellular amastigote stage were BS-1 55.77% at 25 µg/ml, ZI-2 67.78% at 50 µg/ml and again ZI-2 84.93% 100 µg/ml. The highest potency was recorded for BS-1 in both stages, with IC50 values of 9.83 and 4.27 µg/ml against
promastigotes and intracellular amastigotes, respectively. The percent hemolysis as toxicity; the lowest percent hemolysis was recorded for ZI-1 at three different concentrations of 25, 50, 100 µg/ml of 2.60, 3.50, and 6.31, respectively. These results suggested that all the compounds exhibited anti-leishmanial activity, with BS-1 as the most potent. Further studies are suggested to increase the activity of compounds with structural modifications by the addition of some other synergistic, novel, and analogue compounds.