Novel Schiff bases of Vanillin: potent inhibitors of macrophage harbored Leishmania tropica.

Abstract

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 100µg/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 25µg/ml, ZI-2 66.95% at 50µg/ml, and again ZI-2 76.92% at 100µg/ml. Similarly, the highest percent inhibition values against intracellular amastigote stage were BS-1 55.77% at 25µg/ml, ZI-2 67.78% at 50µg/ml and again ZI-2 84.93% 100µg/ml. The highest potency was recorded for BS-1 in both stages, with IC50 values of 9.83 and 4.27µg/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, 100µg/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.