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Chalcone represents a vital biosynthetic scaffold owing to its numerous therapeutic effects. The present study was intended to synthesize 17 chalcone derivatives (-) by direct coupling of substituted acetophenones and benzaldehyde. The target chalcones were characterized by spectroscopic analyses followed by their antimicrobial, and antileishmanial investigations with reference to standard drugs. The majority of the chalcones displayed good to excellent biological activities. Chalcone (1000 µg ml) exhibited the most potent antibacterial effect with its zone of inhibition values of 30, 33 and 34 mm versus , and respectively. The results also confirmed chalcone to be the most potent versus with the lowest IC value of 0.59 ± 0.12 µg ml. Chalcone (500 µg ml) was noticed to be the most potent antifungal agent with its zone of inhibition being 29 mm against . Computational studies of chalcones and supported the preliminary results. The existence of the amino moiety and bromine atom on ring-A and methoxy moieties on ring-B caused better biological effects of the chalcones. In brief, the investigations reveal that chalcones ( and ) can be employed as building blocks to discover novel antimicrobial agents.
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http://dx.doi.org/10.1098/rsos.240410 | DOI Listing |
Mem Inst Oswaldo Cruz
September 2025
Fundação Oswaldo Cruz-Fiocruz, Instituto Oswaldo Cruz, Laboratório Interdisciplinar de Pesquisas Médicas, Rio de Janeiro, RJ, Brasil.
Background: Parasite antigens and plasma lipopolysaccharide (LPS) levels from luminal origin in visceral leishmaniasis (VL) patients are correlated with cellular activation and low CD4+T cell counts.
Objectives: Our aim was to verify whether Leishmania infantum infection damages the intestinal barrier and whether combination antimonial/antibiotic contributes to the reduction of LPS levels and immune activation.
Methods: Golden hamsters were grouped in: G1-uninfected; G2-infected with L.
Chem Biol Drug Des
September 2025
Laboratory of Biochemistry and Animal Toxins, Institute of Biotechnology, Federal University of Uberlandia, Uberlandia, MG, Brazil.
Leishmaniasis, a disease caused by Leishmania parasites, poses a significant health threat globally, particularly in Latin America and Brazil. Leishmania amazonensis is an important species because it is associated with both cutaneous leishmaniasis and an atypical visceral form. Current treatments are hindered by toxicity, resistance, and high cost, driving the need for new therapeutic targets and drugs.
View Article and Find Full Text PDFMar Biotechnol (NY)
September 2025
Faculty of Pharmaceutical Sciences, Tokyo University of Science, Niijuku, Tokyo, Katushika, 125-8585, Japan.
Leishmaniasis is a neglected tropical disease posing significant global health challenges. Given the limited effective treatment options and associated constraints, many patients are unable to complete therapy. In this study, we report the remarkable leishmanicidal activity of onnamides derived from the marine sponge Theonella sp.
View Article and Find Full Text PDFChem Biol Drug Des
August 2025
Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Departamento de Ciências Básica da Saúde, Universidade Estadual de Maringá (UEM), Maringá, Brazil.
Leishmaniasis is one of the most important neglected tropical diseases, prevalent in underdeveloped or developing countries, and new pharmacological agents for this disease are urgently needed. In this study, thiophene derivatives based on the natural product 5'-methyl-(5-[4-acetoxy-1-butynyl])-2,2'-bithiophene were synthesized and evaluated against promastigote forms of Leishmania amazonensis. The bithiophene BT-1 was the most potent and selective synthetic compound toward the parasites, exhibiting IC of 23.
View Article and Find Full Text PDFParasitol Int
February 2026
Manisa Celal Bayar University, Medical Faculty, Department of Parasitology, Manisa, Türkiye.
Cutaneous leishmaniasis (CL) is a neglected tropical disease associated with significant morbidity, primarily due to chronic skin lesions, scarring, and psychosocial consequences. This study aimed to investigate the in vitro and ex vivo antileishmanial effects of thymol (1-500 μM) against Leishmania tropica (MHOM/TR/2012/CBCL-LT) infection. Thymol's in vitro efficacy was assessed on both promastigote (Haemocytometry and CellTiter-Glo assays) and amastigote (Giemsa staining and Parasite Rescue Transformation Assay) forms of L.
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