To synthesize novel more potent trypanocidal and leishmanicidal agents. Hantzsch's synthetic strategy was used to synthesize 1,3-thiazole-4-carboxylates and their -benzylated derivatives. 28 new thiazole-carboxylates and their -benzylated derivatives were established to test their trypanocidal and leishmanicidal activities. From both series, compounds , , , and exhibited a better or comparable trypanocidal profile to benznidazole. Among all tested compounds, was found to be the most potent and was better than benznidazole. Further variation of substituents around 1,3-thiazole-4-carboxylates and or hydrazinyl moiety may assist in establishing better and more potent trypanocidal and leishmanicidal agents.
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http://dx.doi.org/10.4155/fmc-2023-0255 | DOI Listing |
Int J Mol Sci
December 2024
Instituto de Pesquisas de Produtos Naturais Walter Mors (IPPN), Centro de Ciências da Saúde (CCS), Universidade Federal do Rio de Janeiro (UFRJ), Avenida Carlos Chagas Filho, 373, Bloco H, Rio de Janeiro 21941-599, RJ, Brazil.
, a genus within the Malvaceae family, is abundantly distributed in tropical and subtropical areas worldwide. Many species of this genus are widely utilized in various ways, including chewing, in folk medicine, acting as an anti-inflammatory agent, and treating gastrointestinal disorders, rheumatism, and asthma, among other conditions. These applications are largely due to their secondary metabolites, primarily quinolone alkaloids and cyclopeptides.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Laboratory of Planning in Medicinal Chemistry, Department of Pharmaceutical Sciences, Center for Health Sciences, Federal University of Pernambuco, 50740-535, Recife, PE, Brazil. Electronic address:
Trypanosomatidae diseases, such as Chagas disease and leishmaniasis, are caused by protozoan parasites of the Trypanosomatidae family, namely Trypanosoma cruzi and Leishmania species, respectively. There is an urgent need for new therapies. Both pyridine and thiazole rings are recognized as important scaffolds in medicinal chemistry.
View Article and Find Full Text PDFEur J Med Chem
December 2024
National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Inada, Obihiro, Hokkaido, 080-8555, Japan.
Leishmaniasis and trypanosomiasis rank among lethal vector-borne parasitic diseases that are endemic in tropical and sub-tropical countries. There are currently no preventive vaccines against them, and once diagnosed, a handful of less effective drugs clinically accessible are the only therapeutic options offered to treat these ailments. And although curable, the eradication and elimination of these diseases are hampered by the emergence of multidrug-resistant strains of the causal pathogens.
View Article and Find Full Text PDFChem Biodivers
October 2024
Department of Chemistry, Universiade Federal de Minas Gerais, Av. Pres. Antonio Carlos, 6627, Campus Pampulha, CEP 31270-901, Belo Horizonte, MG, Brasil.
Rutaceae Juss. stands out as a botanical family recognized for its remarkable diversity in taxonomy, worldwide distribution, chemical composition, and biological activity exhibited by its compounds. Conchocarpus J.
View Article and Find Full Text PDFExp Parasitol
November 2024
Department of Chemistry, Joseph Sarwuan Tarka University, PMB 2373, Makurdi, Benue State, Nigeria. Electronic address:
Ten compounds, six extracts and five fractions obtained from three Nigerian plants were assayed for their in vitro antitrypanosomal and antileishmanial activities. Each plant was extacted with hexane, ethyl acetate, and methanol. Isolated compounds were characterized and identified based on their NMR chemical shifts and comparison to literature reports.
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