Several bicyclic amides and esters of dialkylamino acids were prepared. Their activities against a multiresistant strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900) were examined. Structure-activity relationships were discussed. Particularly the ester compounds showed good antiplasmodial and antitrypanosomal activity and a single compound was tested in vivo against Plasmodium berghei.
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http://dx.doi.org/10.1016/j.bmc.2009.04.002 | DOI Listing |
Angew Chem Int Ed Engl
September 2024
Max-Planck-Institut für Kohlenforschung, 45470, Mülheim/Ruhr, Germany.
The strasseriolide macrolides show promising in vitro and in vivo activities against P. falciparum and T. cruzi, the parasites causing malaria and Chagas disease, respectively.
View Article and Find Full Text PDFInt J Mol Sci
April 2024
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d'Alcontres, 98166 Messina, Italy.
In recent decades, neglected tropical diseases and poverty-related diseases have become a serious health problem worldwide. Among these pathologies, human African trypanosomiasis, and malaria present therapeutic problems due to the onset of resistance, toxicity problems and the limited spectrum of action. In this drug discovery process, rhodesain and falcipain-2, of and , are currently considered the most promising targets for the development of novel antitrypanosomal and antiplasmodial agents, respectively.
View Article and Find Full Text PDFHandb Exp Pharmacol
March 2024
Guangxi Key Laboratory of Marine Natural Products and Combinatorial Biosynthesis Chemistry, Guangxi Academy of Marine Sciences, Guangxi Academy of Sciences, Nanning, Guangxi, China.
Parasitic diseases including malaria, leishmaniasis, and trypanosomiasis have received significant attention due to their severe health implications, especially in developing countries. Marine natural products from a vast and diverse range of marine organisms such as sponges, corals, molluscs, and algae have been found to produce unique bioactive compounds that exhibit promising potent properties, including antiparasitic, anti-Plasmodial, anti-Leishmanial, and anti-Trypanosomal activities, providing hope for the development of effective treatments. Furthermore, various techniques and methodologies have been used to investigate the mechanisms of these antiparasitic compounds.
View Article and Find Full Text PDFHeliyon
December 2023
Department of Organic Chemistry, Faculty of Science, University of Yaoundé 1, P.O. Box 812, Yaoundé, Cameroon.
BMC Complement Med Ther
December 2023
Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Kasr-El-Ainy Street, Cairo, 11562, Egypt.
Background: In the last few decades, the use of plant extracts and their phytochemicals as candidates for the management of parasitic diseases has increased tremendously. Irises are aromatic and medicinal plants that have long been employed in the treatment of different infectious diseases by traditional healers in many cultures. This study aims to explore the potential of three common Iris species (I.
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