We aim to develop new anti-leishmanial agents against and . A total of 23 thiourea derivatives of (±)-aminoglutethimide were synthesized and evaluated for activity against promastigotes of and . The -benzoyl analogue was found potent (IC = 12.7 μM) against and non toxic to normal cells. The docking studies, indicates that these inhibitors may target folate and glycolytic pathways of the parasite. The -hexyl compound was found strongly active against both species, and lacked cytotoxicity against normal cells, whereas compound , with a 3,5-bis-(tri-fluoro-methyl)phenyl unit, was active against , but was cytotoxic in nature. Compound was thus identified as a hit for further studies.
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http://dx.doi.org/10.1080/17568919.2024.2359362 | DOI Listing |
Mini Rev Med Chem
January 2025
Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru 81310, Johor, Malaysia.
Indole, a ubiquitous structural motif in bioactive compounds, has played a pivotal role in drug discovery. Among indole derivatives, indole-3-carboxaldehyde (I3A) has emerged as a particularly promising scaffold for the development of therapeutic agents. This review delves into the recent advancements in the chemical modification of I3A and its derivatives, highlighting their potential applications in various therapeutic areas.
View Article and Find Full Text PDFPharmaceuticals (Basel)
November 2024
Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, Rio de Janeiro 21040-900, Brazil.
Leishmaniasis, caused by protozoa and transmitted by vectors, presents varied clinical manifestations based on parasite species and host immunity. The lack of effective vaccines or treatments has prompted research into new therapies, including thiourea derivatives, which have demonstrated antiprotozoal activities. We synthesized two series of ,'-disubstituted thiourea derivatives through the reaction of isothiocyanates with amines.
View Article and Find Full Text PDFSci Rep
December 2024
Department of Statistics, College of Natural and Computational Sciences, Gambella University, Gambella, Ethiopia.
Visceral leishmaniasis (VL) is a neglected tropical disease that mostly affects the working-class and impoverished segments of society, having a significant negative effect on the economic development of the affected nation. While anti-leishmanial medications lower mortality among VL patients, patients may still die or require more time to recover (TTR) while receiving treatment. In this regard, there are limited studies in Ethiopia.
View Article and Find Full Text PDFIn Silico Pharmacol
December 2024
Laboratory of Cell and Molecular Biology, Department of Botany, Centre of Advanced Study, University of Calcutta, 35 Ballygunge Circular Road, Kolkata, 700019 India.
Visceral Leishmaniasis, caused by is the second most deadly parasitic disease, causing over 65,000 deaths annually. Synthetic drugs available in the market, to combat this disease, have numerous side effects. In this backdrop, we aim to find safer antileishmanial alternatives with minimal side effects from mushrooms, which harbour various secondary metabolites with promising efficacy.
View Article and Find Full Text PDF3 Biotech
January 2025
Cell and Molecular Biology Laboratory, Department of Zoology, Soban Singh Jeena University, Campus Almora, Almora, Uttarakhand India.
Unlabelled: Visceral leishmaniasis (VL), caused by , remains challenging to treat due to severe side effects and increasing drug resistance associated with current chemotherapies. Our study investigates the anti-leishmanial potential of from Uttarakhand, India, with extracts prepared from leaves and stems using ethanol and hexane. Advanced GC-MS analysis identified over 100 bioactive compounds, which were screened using molecular docking to assess their binding to LdHEL-67, a DDX3-DEAD box RNA helicase of donovani.
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