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Molecules 2015, 20(12), 22435-22444; doi:10.3390/molecules201219857

The Antileishmanial Potential of C-3 Functionalized Isobenzofuranones against Leishmania (Leishmania) Infantum Chagasi

1
Departamento de Química, Universidade Federal de Viçosa, Av. P.H. Rolfs, S/N, Viçosa, MG, 36.570-900, Brazil
2
Departamento de Biologia Geral, Universidade Federal de Viçosa, Av. P.H. Rolfs, S/N, Viçosa, MG, 36.570-900, Brazil
3
Instituto Nacional de Biotecnologia Estrutural e Química Medicinal em Doenças Infecciosas (INBEQMeDi), Instituto de Física de São Carlos, Av. Trabalhador São Carlense, 400, Caixa Postal 369, São Carlos, SP, 13.560-970, Brazil
4
Departamento de Ciências Biológicas, Instituto de Ciências Exatas e Biológicas—ICEB/NUPEB, Campus do Morro do Cruzeiro, Universidade Federal de Ouro Preto, Ouro Preto, MG, 35.400-000, Brazil
5
Departamento de Veterinária, Universidade Federal de Viçosa, Av. P.H. Rolfs, S/N, Viçosa, MG, 36.570-900, Brazil
6
Departamento de Bioquímica e Biologia Molecular, Av. P.H. Rolfs, S/N, Viçosa, MG, 36.570-900, Brazil
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 5 November 2015 / Revised: 3 December 2015 / Accepted: 8 December 2015 / Published: 14 December 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2319 KB, uploaded 14 December 2015]   |  

Abstract

Leishmaniases are diseases caused by protozoan parasites of the genus Leishmania. Clinically, leishmaniases range from cutaneous to visceral forms, with estimated global incidences of 1.2 and 0.4 million cases per year, respectively. The treatment of these diseases relies on multiple parenteral injections with pentavalent antimonials or amphotericin B. However, these pharmaceuticals are either too toxic or expensive for routine use in developing countries. These facts call for safer, cheaper, and more effective new antileishmanial drugs. In this investigation, we describe the results of the assessment of the activities of a series of isobenzofuran-1(3H)-ones (phtalides) against Leishmania (Leishmania) infantum chagasi, which is the main causative agent of visceral leishmaniasis in the New World. The compounds were tested at concentrations of 100, 75, 50, 25 and 6.25 µM over 24, 48, and 72 h. After 48 h of treatment at the 100 µM concentration, compounds 7 and 8 decreased parasite viability to 4% and 6%, respectively. The concentration that gives half-maximal responses (LC50) for the antileishmanial activities of compounds 7 and 8 against promastigotes after 24 h were 60.48 and 65.93 µM, respectively. Additionally, compounds 7 and 8 significantly reduced parasite infection in macrophages. View Full-Text
Keywords: Leishmania (L.) infantum chagasi; visceral leishmaniasis; isobenzofuranones; phthalides; in vitro leishmanicidal activity Leishmania (L.) infantum chagasi; visceral leishmaniasis; isobenzofuranones; phthalides; in vitro leishmanicidal activity
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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. (CC BY 4.0).

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MDPI and ACS Style

Pereira, W.L.; de Souza Vasconcellos, R.; Mariotini-Moura, C.; Saar Gomes, R.; Firmino, R.C.; da Silva, A.M.; Silva Júnior, A.; Bressan, G.C.; Almeida, M.R.; Crocco Afonso, L.C.; Teixeira, R.R.; Lopes Rangel Fietto, J. The Antileishmanial Potential of C-3 Functionalized Isobenzofuranones against Leishmania (Leishmania) Infantum Chagasi. Molecules 2015, 20, 22435-22444.

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