A series of 2-(1-methyl-5-nitroimidazol-2-yl)-5-(1-piperazinyl, 1-piperidinyl and 1-morpholinyl)-1,3,4-thiadiazoles (3a-g) were synthesized and evaluated for in vitro leishmanicidal activity against Leishmania major promastigotes. The leishmanicidal data revealed that compounds 3a-g had strong and much better leishmanicidal activity than the reference drug pentostam. Compound 3c (piperazine analog) was the most active compound (IC50=0.19 microM).
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http://dx.doi.org/10.1016/j.ejmech.2005.07.002 | DOI Listing |
Chem Biodivers
January 2025
Universidade Federal de Pernambuco Centro de Biociencias, Centro de Biociências, Av. Prof. Moraes Rego, 1235 - Cidade Universitária, Recife - PE, 50670-901, 50670-901, Recife, BRAZIL.
Leishmaniasis is a neglected disease caused by parasites of the genus Leishmania sp. that causes approximately 1 million cases and 650,000 deaths annually worldwide. Its treatment has several limitations mainly due to high toxicity and clinical resistance, and the search for alternatives is highly desirable.
View Article and Find Full Text PDFInt 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
February 2025
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 PDFBioorg Chem
January 2025
Universidad de Buenos Aires, CONICET, Cátedra de Química Orgánica II, Departamento de Ciencias Químicas, Facultad de Farmacia y Bioquímica, Junín 956, 1113 Buenos Aires, Argentina. Electronic address:
Arch Biochem Biophys
February 2025
Department of Biochemistry and Immunology, Ribeirão Preto Medical School, University of São Paulo, Ribeirão Preto, Brazil. Electronic address:
UBC13 is an orthologue of Homo sapiens ubiquitin-conjugation E2 enzymes described in Leishmania mexicana, a null mutant lacking this gene cannot be produced, suggesting essential functions in this parasite. Leishmania infantum is an etiological agent of visceral leishmaniasis, the most severe type of disease that is potentially fatal if untreated. The ubiquitination process has been targeted for leishmanicidal compounds, indicating its essential function in parasite homeostasis.
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