Antiprotozoal action of synthetic cinnamic acid analogs

Abstract

Introduction: Leishmaniasis, Chagas disease, and malaria cause morbidity globally. The drugs currently used for treatment have limitations. Activity of cinnamic acid analogs against Leishmania spp., Trypanosoma cruzi, and Plasmodium falciparum was evaluated in the interest of identifying new antiprotozoal compounds. Methods: In vitro effects of analogs against L. braziliensis, L. infantum chagasi, T. cruzi, and P. falciparum, and hemolytic and cytotoxic activities on NCTC 929 were determined. Results: Three analogs showed leishmanicidal and tripanocidal activity. No antiplasmodial, hemolytic, or cytotoxic activity was observed. Conclusions: Antiprotozoal activity of analogs against L. infantum braziliensis, L. infantum chagasi, and T. cruzi was demonstrated.

Cinnamic Acid Conjugates in the Rescuing and Repurposing of Classical Antimalarial Drugs

“…Therefore, this work conveyed the disclosure of CAD as inhibitors of the new permeability pathways (NPP) induced by Plasmodium in erythrocytes to enable the translocation of carbohydrates and amino acids [46][47][48][49]. Following this pioneering discovery, other authors have proposed different CA-inspired compounds as potential therapeutic agents against malaria [26,28,29], as well as other parasitic diseases [50][51][52]. In view of this, reports have emerged over the past decade where conjugation to CA was proposed as a useful strategy for the rescuing of known antimalarials [53][54][55].…”

“…Molecules 2020, 24, x FOR PEER REVIEW 3 of 15 malaria [26,28,29], as well as other parasitic diseases [50][51][52]. In view of this, reports have emerged over the past decade where conjugation to CA was proposed as a useful strategy for the rescuing of known antimalarials [53][54][55].…”

Synthesis of Esters Containing Cinnamoyl Motif with Potential Larvicide Action: A Computational, Ecotoxicity and in Vitro Cytotoxicity Assessments

“…The CADs have also exhibited inhibitory effects against parasites transmitted by infected mosquitoes, such as the malaria-causing protozoa. [18] Ruwizhi and Aderibigbe demonstrated the antiparasitic function against leishmaniasis ascribed to CADs hybridized with triazole moieties. [19] Likewise, it is reported the insecticidal action of CADs against Tuta absoluta larvae is related to ethyl cinnamates and propyl cinnamate.…”

In vitro and ex vivo antiplasmodial activity of 1-(3-benzyloxy-4-methoxy-phenyl)-3-(3,4,5-trimethoxy-phenyl)-propan-1-one) against circulating strains of Plasmodium spp. in the state of Rondônia, Brazil

“…In this context, we can highlight plants of the genus Piper L., Piperaceae which have components such as: amides, alkaloids, derivatives of benzoic acid, lignans, flavonoids and cinnamic acid (Facundo et al, 2008;Regasini et al, 2009). There are reports in the literature of trypanocidal, leishmanicidal and anti-inflammatory bioactivity for this genus (Calderon et al, 2009;Santos et al, 2018;Oliveira et al, 2018). In addition, there are other studies and reviews published in the literature demonstrating specific action of molecules derived from cinnamic acid (Guzman, 2014).…”

“…The compounds that make up this family of metabolites were extracted, modified and synthesized for future studies. Santos et al (2018) demonstrated that synthetic compounds derived from trimethoxyphenylpropanoic acid showed antiprotozoal action against Leishmania spp. and T. cruzi; study conducted by Ferreira et al (2010) also reinforced the 3,4,5-trimethoxyphenyl group's activity.…”