Synthesis and biological evaluation against Leishmania amazonensis of a series of alkyl-substituted benzophenones |
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| Authors: | Claudia Mara Maciel-Rezende Letícia de Almeida Éderson D’Martin Costa Francieli Ribeiro Pires Karina Ferreira Alves Cláudio Viegas Junior Danielle Ferreira Dias Antônio Carlos Doriguetto Marcos José Marques Marcelo Henrique dos Santos |
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| Institution: | 1. Laboratório de Fitoquímica e Química Medicinal–LFQM, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil;2. Programa de Pós-Graduação em Química, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil;3. Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil;4. Laboratório de Biologia Molecular de Microrganismos, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil;5. Instituto de Química, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil;6. Instituto de Ciências Biomédicas, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil;7. Faculdade de Farmácia, Universidade Federal de Alfenas, 37130-000 Alfenas, MG, Brazil |
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| Abstract: | Nine O-alkyl and O-prenyl derivatives were synthesized from commercial 2,4-dihydroxybenzophenone, 4,e4,4′-dihydroxybenzophenone and were evaluated for their leishmanicidal activity against promastigote forms of Leishmania amazonensis, as well their toxicity in murine macrophages. All derivatives exhibited better biological activity than their hydroxylated benzophenones precursors, and new compound LFQM-123 (3c) was 250-fold more active than its precursor 4,4′-dihydroxybenzophenone (3). Moreover, some of the results were comparable to the standard drug Amphotericin B, suggesting that the increase in lipophilicity could facilitate protozoa membrane permeation. In this study we confirmed that benzophenone derivatives exhibit leishmanicidal properties, with relatively low toxicity, and thus could be exploited as promise prototypes for the design and development of new drug for the treatment of leishmaniasis. |
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| Keywords: | Benzophenone derivatives Leishmaniasis |
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