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This study focused on the synthesis, antimicrobial, and antileishmanial evaluation of seven amide derivatives ( to ). The target compounds were synthesized from cysteine methyl ester and various substituted aromatic and aliphatic carboxylic acids. The final products were characterized using physical and spectro-analytical techniques (FT-IR, H NMR). The derivatives were evaluated for their antimicrobial activity at various concentrations. Experimental studies revealed that compounds and were the most potent against and , exhibiting 18 mm and 21 mm inhibition zones, respectively, at a concentration of 2000 µg/mL. Additionally, and showed significant activity against , with 20 mm and 23 mm inhibition zones, respectively, at a concentration of 1000 µg/mL. The compounds also exhibited moderate to good activity against . Compounds , and demonstrated good activity, with IC values of 0.68 ± 0.09, 0.68 ± 0.16, 0.66 ± 0.08, and 0.68 ± 0.12 µg/mL, respectively. Molecular docking, Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) analysis, and Density Functional Theory (DFT) studies were conducted on the most potent compounds ( and ) to validate and support their experimental antimicrobial and antileishmanial potential.
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http://dx.doi.org/10.1080/17568919.2025.2479419 | DOI Listing |
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.
View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
August 2025
Departamento de Ciencias Biomédicas, Facultad de Veterinaria, Universidad de León, Campus de Vegazana s/n, 24007, León, Spain; Instituto de Biomedicina (IBIOMED), Universidad de León, Campus de Vegazana s/n, 24007, León, Spain. Electronic address:
Visceral leishmaniasis caused by Leishmania infantum and Leishmania donovani is one of the neglected tropical diseases (NTDs) caused by trypanosomatids with treatment options limited to outdated drugs often causing adverse effects and promoting drug resistance. Previous antileishmanial drug discovery campaigns have identified nitroheterocyclic molecules with high efficacy and a high selectivity index. Therefore, we have evaluated on our screening platform of fluorescent L.
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