This work describes a systematic and bibliometric review of the factors that contribute to the expansion of leishmaniasis in urban areas. Three scientific databases were used: (Sci), and , encompassing all original and review articles between 1959 and 2021. Three descriptors were used: "leishmaniasis" AND "urban" AND "rural.
View Article and Find Full Text PDFWithin this work, we describe the design and synthesis of a range of novel thiochromanones based on natural products reported to possess anti-leishmanial action, and their synthetic derivatives. All compounds were elaborated via the key intermediate 2,2,6-trimethoxythiochromanone, which was modified at the benzylic position to afford various ester, amine and amide analogues, substituted by chains of varying lipophilicity. Upon testing in , IC values revealed the most potent compounds to be phenylalkenyl and haloalkyl amides and , with IC values of 10.
View Article and Find Full Text PDFWithin this work, we describe the design and synthesis of a range of novel chromanones and quinolinones, based on natural products reported to possess anti-leishmanial action. The core heterocycles were obtained either via classical or ionic liquid mediated Kabbe condensation in the case of chromanones, or aqueous Sonogashira based alkynylation followed by acid-catalysed cyclisation in the case of quinolinones. Upon testing in promastigotes, axenic amastigotes and -infected macrophages, compound was identified as displaying interesting activity, inhibiting axenic amastigotes and intracellular amastigotes with ICs of 25.
View Article and Find Full Text PDFSprengel, popularly known as "guaco," is used in Brazilian folk medicine for several inflammatory and allergic conditions. Besides, the popular use "guaco" is indicated by the Brazilian Ministry of Health as a safe and effective herbal medicine. The biological activity of extracts is due to the presence of the coumarins, a large family of phenolic substances found in plants and is made of fused benzene and α-pyrone rings.
View Article and Find Full Text PDFChagas disease, caused by Trypanosoma cruzi, affects millions of people in South America and no satisfactory therapy exists, especially for its life threatening chronic phase. We targeted the Proline Racemase of T. cruzi, which is present in all stages of the parasite life cycle, to discover new inhibitors against this disease.
View Article and Find Full Text PDFA new approach to the total synthesis of (-)-epimyrtine has been developed from D-alanine. The key step to access the enantiopure pyridone intermediate was achieved by a gold-mediated cyclization. Finally, various transformations afforded the natural product in a few steps and good overall yield.
View Article and Find Full Text PDFMedicinal plants are still widely used worldwide; yet for some species, little or no information is available concerning their biological activity, specially their genotoxic and antimutagenic potential. Mikania laevigata (Asteraceae) is a native plant from South America, and its extracts are largely used to treat respiratory complaints. The aim of the present work was then to evaluate, in vivo, the potential biological activity of M.
View Article and Find Full Text PDFBackground: Kavalactones are pharmacologically active compounds present in preparations of the root trunk of Piper methysticum Forst, known as kava. This work describes the analgesic activity of some synthesized analogues of synthetic kavain, which is the main component of kava.
Methods: The essays were initially performed against the writhing test in mice, and the most promising compound was analyzed using other classical models of nociception, including formalin-, capsaicin-, glutamate-induced nociception, the hot plate test, and measurement of motor performance.
Melissa officinalis (L.) (Lamiaceae), a plant known as the lemon balm, is native to the east Mediterranean region and west Asia. Also found in tropical countries, such as Brazil, where it is popularly known as "erva-cidreira" or "melissa", it is widely used in aqueous- or alcoholic-extract form in the treatment of various disorders.
View Article and Find Full Text PDFPurpose: A series of delta-valerolactones has been synthesized in good yields, by reaction of ethyl acetoacetate with several aldehydes in presence of LDA.
Methods And Results: The in vivo analgesic activity of these compounds has been evaluated. The results indicate that the lactones synthesized showed an important antinociceptive effect at 10 mg/kg, administered intraperitoneally in mice, which significantly inhibited the abdominal constrictions induced by acetic acid when compared to acetylsalicylic acid and acetaminophen in the same dose, and increased significantly the thermal sensibility at the hot-plate method, although they were less effective than morphine in the same assay.