Targeting Leishmania with Nitrovinyl Derivatives: Synthesis, in Vitro Assessment, and Computational Exploration
26 Pages Posted: 20 Mar 2024
Abstract
Leishmaniasis is an affliction attributed to the protozoan parasites within the Leishmania genus. This disorder impacts a substantial global populace, exceeding one million individuals, leading to disability-adjusted life years and fatalities, particularly within tropical regions. At present, the existing drug therapies have not attained a degree of efficacy that can be unequivocally classified as genuinely triumphant. The notable limitations encompassing irritating side effects, pronounced toxicity, elevated costs, prolonged treatment durations, discomforting injections, and the emergence of drug resistance collectively stand out as significant impediments. In this context, the conception of novel compounds possessing the capacity to impede the parasite's life cycle at various stages holds considerable significance. In this research endeavor, an exploration was undertaken involving the design and synthesis of nineteen derivatives incorporating the nitrovinyl pharmacophore. The subsequent evaluation of their impacts on L. major was conducted through a combination of in vitro and in silico (molecular docking) investigations.
Note:
Funding declaration: The authors would like to acknowledge the support of Kerman University of Medical Sciences (KMU) Research Vice-Chancellor for this project (Reg. No. = 401000464 and and
ethical approval: IR.KMU.REC.1401.423.)
Conflict of Interests: The authors declared no potential conflicts of interest with respect to the research, authorship, and/or publication of this article.
Keywords: : Nitrovinyl, Anti-leishmania, Amastigote, Promastigote, Leishmania major, Molecular docking
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