Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Selenium-Containing (Hetero)Aryl Hybrids as Potential Antileishmanial Drug Candidates: In vitro Screening Against L. amazonensis

Maria Helena Fermiano
ORCID logo ,
Amarith Rodrigues Das Neves
,
Fernanda Da Silva
,
Manuella Salustiano Andrade Barros
,
Camila Barbosa Vieira
,
André L. Stein
,
Tiago Elias Allievi Frizon
,
Antonio Luiz Braga
ORCID logo ,
Carla Cardozo Pinto De Arruda
ORCID logo ,
Eduardo Benedetti Parisotto
ORCID logo ,
Sumbal Saba
,
Jamal Rafique
* ORCID logo ,
Thalita Bachelli Riul
* ORCID logo
Version 1 : Received: 20 December 2023 / Approved: 21 December 2023 / Online: 21 December 2023 (16:01:01 CET)

A peer-reviewed article of this Preprint also exists.

Fermiano, M.H.; das Neves, A.R.; da Silva, F.; Barros, M.S.A.; Vieira, C.B.; Stein, A.L.; Frizon, T.E.A.; Braga, A.L.; de Arruda, C.C.P.; Parisotto, E.B.; Saba, S.; Rafique, J.; Riul, T.B. Selenium-Containing (Hetero)Aryl Hybrids as Potential Antileishmanial Drug Candidates: In Vitro Screening against L. amazonensis. Biomedicines 2024, 12, 213. Fermiano, M.H.; das Neves, A.R.; da Silva, F.; Barros, M.S.A.; Vieira, C.B.; Stein, A.L.; Frizon, T.E.A.; Braga, A.L.; de Arruda, C.C.P.; Parisotto, E.B.; Saba, S.; Rafique, J.; Riul, T.B. Selenium-Containing (Hetero)Aryl Hybrids as Potential Antileishmanial Drug Candidates: In Vitro Screening against L. amazonensis. Biomedicines 2024, 12, 213.

Abstract

Leishmaniasis remains a significant global health concern, with current treatments relying on outdated drugs associated with high toxicity, lengthy administration, elevated costs, and drug resistance. Consequently, the urgent need for safer and more effective therapeutic options in leishmaniasis treatment persists. Previous research has highlighted selenium compounds as promising candidates for innovative leishmaniasis therapy. In light of this, a library of 10 selenium-containing diverse compounds was designed and evaluated in this study. The compounds were subjected to screening against L. amazonensis promastigotes, and their cytotoxicity was assessed in NIH/3T3 cells. Among the tested compounds, MRK-106 and MRK-108 displayed the highest potency against L. amazonensis promastigotes while demonstrating reduced cytotoxicity. Notably, MRK-106 and MRK-108 exhibited IC50 values of 3.97 µM, 4.23 µM, respectively, and most of the tested compounds showed low cytotoxicity in NIH/3T3 cells (CC50 > 200 µM). Although these results are promising, additional investigations focusing on intracellular amastigotes are required to determine the antileishmanial activity of the compounds. In conclusion, the identified selenium-containing compounds hold considerable potential as antileishmanial drug candidates and warrant further exploration in subsequent studies. These findings represent a significant step towards the development of safer and more effective therapies for leishmaniasis, addressing the pressing need for novel and improved treatments.

Keywords

leishmaniasis; selenide; 2,5-dihydrooxazole; indole; chromone; coumarin; β-naphthol; 1,3,4-oxadiazole; imidazo[1,2-a]pyridine; imidazo[2,1-b]thiazole

Subject

Medicine and Pharmacology, Other

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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