Chagas Disease and Coumarins: A Review of Natural and Synthetic Coumarins As Anti-Trypanosoma Cruzi Agents

Abstract

The complexity of Chagas disease is still a challenge in endemic regions and an emergent public health problem in non-endemic countries. The causative agent of this neglected tropical disease, Trypanosoma cruzi, is mainly transmitted by triatomine vectors and possesses multiple epidemiologically important strains. Current chemotherapeutics are outdated and their limited efficacy is one of the major reasons for treatment discontinuation. In this context, it is urgent the development of novel, safe and economically accessible antichagasic drugs. Various classes of heterocycles and natural compounds have been described as potential antichagasic scaffolds, and coumarins are no exception. These versatile compounds have a wide spectrum of biological activities, and numerous natural and synthetic coumarins have been reported with antichagasic potential. The aim of this review is to discuss the available literature between 2001 and 2020 regarding natural and synthetic coumarins with anti-Trypanosoma cruzi activity. Moreover, some of the studies herein comprised are dedicated to the potential of coumarins to inhibit promising targets in Trypanosoma cruzi.

Antiproliferative activity and toxicity evaluation of 1,2,3-triazole and 4-methyl coumarin hybrids in the MCF7 breast cancer cell line

“…Currently, the bicyclic coumarin skeleton is considered by medicinal chemists as a privileged structure because of its wide array of biological properties reported in the literature such as being an antioxidant, 2,3 anti-inflammatory, 4,5 antiviral, 6 antibacterial, 7 an acetylcholinesterase inhibitor, 8,9 antileishmanial 10 and against Chagas disease. 11 The first coumarins to enter the pharmaceutical market were dicumarol 1 and warfarin 2 in the 1950s, as anticoagulants. More recently, irosustat 3 , an orally active, irreversible steroid sulfatase inhibitor coumarin, reached clinical trials for endometrial cancer.…”

Coumarin-based derivatives targetingTrypanosoma cruzicruzain andTrypanosoma bruceicathepsin L-like proteases

“…[28][29][30] Among them, coumarins have emerged as promising and versatile scaffolds to design and develop novel trypanocidal agents. 31,32 Brak et al 33 synthesized 1,4-disubstituted-1,2,3-triazoles attached to fluoro-7-amino-4-methyl coumarin acetic acid (AMCA) to identify agents against CRZ. Among them, derivatives containing quinoline (1) and benzothiazole (2) cores (Fig.…”

Synthesis and Characterization of a Coumarin Antimicrobial Polymer Fluorescent Coating

“…Coumarin is a natural antibacterial compound with fluorescence, and its derivatives have a variety of biological and physicochemical properties such as antibacterial, antifungal, and insecticidal [12][13][14][15]. In addition, coumarin diffraction materials have been widely studied and applied in many fields, such as fluorescence labels, fluorescence images, nonlinear optical chromophores, fluorescence probes, and laser dyes, because of their high emissivity, wide spectral range, and excellent optical stability [16][17][18][19][20].…”