Targeting Leishmania with Nitrovinyl Derivatives: Synthesis, in Vitro Assessment, and Computational Exploration

26 Pages Posted: 20 Mar 2024

See all articles by Ali Asadipour

Ali Asadipour

Kerman University of Medical Sciences

Fatemeh Ghelich Khani

Kerman University of Medical Sciences

Fatemeh Sharifi

Kerman University of Medical Sciences - Infectious and Tropical Research Center

Mohammad Amin Langarizadeh

Kerman University of Medical Sciences

Ehsan Salarkia

Kerman University of Medical Sciences - Leishmaniasis Research Center

Marziye Ranjbar Tavakoli

Kerman University of Medical Sciences

Bagher amirheidari

Kerman University of Medical Sciences

Mehdi Ranjbar

Kerman University of Medical Sciences

Ehsan Faghih-mirzaei

Kerman University of Medical Sciences

yaghoub pourshojaei

Kerman University of Medical Sciences

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

Suggested Citation

Asadipour, Ali and Ghelich Khani, Fatemeh and Sharifi, Fatemeh and Langarizadeh, Mohammad Amin and Salarkia, Ehsan and Ranjbar Tavakoli, Marziye and amirheidari, Bagher and Ranjbar, Mehdi and Faghih-mirzaei, Ehsan and pourshojaei, yaghoub, Targeting Leishmania with Nitrovinyl Derivatives: Synthesis, in Vitro Assessment, and Computational Exploration. Available at SSRN: https://ssrn.com/abstract=4758152 or http://dx.doi.org/10.2139/ssrn.4758152

Ali Asadipour

Kerman University of Medical Sciences ( email )

Kerman
Iran

Fatemeh Ghelich Khani

Kerman University of Medical Sciences ( email )

Kerman
Iran

Fatemeh Sharifi

Kerman University of Medical Sciences - Infectious and Tropical Research Center ( email )

Mohammad Amin Langarizadeh

Kerman University of Medical Sciences ( email )

Kerman
Iran

Ehsan Salarkia

Kerman University of Medical Sciences - Leishmaniasis Research Center ( email )

Marziye Ranjbar Tavakoli

Kerman University of Medical Sciences ( email )

Kerman
Iran

Bagher Amirheidari

Kerman University of Medical Sciences ( email )

Kerman
Iran

Mehdi Ranjbar

Kerman University of Medical Sciences ( email )

Kerman
Iran

Ehsan Faghih-mirzaei

Kerman University of Medical Sciences ( email )

Kerman
Iran

Yaghoub Pourshojaei (Contact Author)

Kerman University of Medical Sciences ( email )

Kerman
Iran

Do you have a job opening that you would like to promote on SSRN?

Paper statistics

Downloads
49
Abstract Views
166
PlumX Metrics