Amidines: The Main Discoveries in the Synthesis and Anti-Leishmanial Effects of New Chemotherapeutic Agents

Leishmaniasis is an infectious disease caused by protozoan parasites of the Leishmania genus and affects more than 90 countries, especially in tropical and subtropical regions. The first treatment for these diseases involves pentavalent antimonial derivatives, which are very toxic and cause severe side effects. The other chemotherapeutic drugs used as second-line agents include different organic compound classes, such as pentamidine, which also cause severe side effects. Thus, new, safer, and efficient antileishmaniasis agents are urgently needed to control and treat these diseases. This mini review, which considered the last two decades of related research, highlighted the principal synthetic methodologies used to access amidine derivatives, focusing on more eco-friendly methods. Furthermore, the results obtained from evaluations of the anti-Leishmania activity and several molecular targets of the amidine derivatives are highlighted.

Keywords:
leishmaniasis; trypanosomatids; amidine derivatives; chemotherapy; tropical disease

Authorship

Cláudio E. Rodrigues-Santos

Cláudio E. Rodrigues-Santos received his bachelor’s and teaching degree in Chemistry in 2002, and he obtained his MSc (2002) and PhD (2008) in Science from the Rural University of Rio de Janeiro. Currently, he is an Associate Professor in the Department of Organic Chemistry of the Rural University of Rio de Janeiro. His research interests are focused on the synthesis of pyrazolo[3,4-b]pyridin-6-ones, 4-aryl-3,4-dihydrocoumarins, amidines, the development of green protocols, microwave and ultrasound utilization, and the planning of bioactive molecules. Recently, he has been working to develop new teaching methodologies.

Instituto de Química, Universidade Federal Rural do Rio de Janeiro, 23890-000 Seropédica-RJ, BrazilUniversidade Federal Rural do Rio de JaneiroBrazilSeropédica, RJ, BrazilInstituto de Química, Universidade Federal Rural do Rio de Janeiro, 23890-000 Seropédica-RJ, Brazil

https://orcid.org/0000-0003-0129-2802

Maurício R. de Brito

Maurício R. de Brito is an MSc Student at UFRRJ Chemistry Post Degree Program (Seropédica, Rio de Janeiro State, Brazil) and opted for the emphasis on materials chemistry. He also holds a bachelor’s degree in Chemical Engineering (UFRRJ) and acts as a temporary researcher in the UFRRJ Chemistry Institute’s photochemistry and photocatalysis group. His major interests are organic synthesis, theoretical chemistry, and photochemistry.

Aurea Echevarria ^** e-mail: claudioers@ufrrj.br; echevarr@ufrrj.br

Aurea Echevarria is a Professor of Organic Chemistry at the Universidade Federal Rural do Rio de Janeiro (UFRRJ, Brazil). She is graduated and Master in Chemistry at Universidade Estadual de Campinas (UNICAMP, Brazil), and obtained a doctorate degree in Organic Chemistry at Universidade de São Paulo (USP, Brazil) working on physical organic chemistry involving mesoionic compounds (1986). She subsequently completed a postdoctorate at the Instituto de Química Medica (CSIC, Madrid). In fact, she has developed projects in medicinal chemistry involving cancer and neglected diseases, as well as new organic materials.

https://orcid.org/0000-0002-7330-676X

* e-mail: claudioers@ufrrj.br; echevarr@ufrrj.br

Editor handled this article: Brenno A. D. Neto

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