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Acetyl CoA synthetases (ACS) have emerged as drug targets for the treatment of cancer, metabolic diseases as well as fungal and parasitic infections. Although a variety of small molecule ACS inhibitors have been discovered, the systematic optimization of these molecules has been slowed by a lack of structural information regarding their mechanism of inhibition. Through a chemical genetic-based, synthetic lethal screen of the human fungal pathogen Cryptococcus neoformans, we identified an isoxazole-based ACS inhibitor with antifungal activity and exquisite selectivity for the C.
View Article and Find Full Text PDFMalaria prevalence, transmission potential and efficacy of artemisinin-based combination therapy in the Kenyan Central highlands: a zone previously characterized as malaria-free.
Malar J
January 2025
Centre for Biotechnology Research and Development, Kenya Medical Research Institute (KEMRI), Nairobi, Kenya.
Background: The current study sought to re-evaluate malaria prevalence, susceptibility to artemisinin-based combination therapy (ACT), transmission patterns and the presence of malaria vectors in the Kikuyu area of the Kenyan Central highlands, a non-traditional/low risk malaria transmission zone where there have been anecdotal reports of emerging malaria infections.
Methods: Sampling of adult mosquitoes was done indoors, while larvae were sampled outdoors in June 2019. The malaria clinical study was an open label non-randomized clinical trial where the efficacy of one ACT drug, was evaluated in two health facilities.
Hydroxychloroquine-induced Sweet's Syndrome: A Case Report and Literature Review.
Acta Derm Venereol
January 2025
Dermatology Department, Unidade Local de Saúde Santa Maria, Lisbon, Portugal; Dermatology University Clinic, Faculty of Medicine, University of Lisbon, Lisbon, Portugal; Dermatology Research Unit, Instituto de Medicina Molecular, University of Lisbon, Lisbon, Portugal.
Sweet's syndrome (or acute febrile dermatosis) is a neutrophilic dermatosis with a characteristic presentation encompassing specific clinical (fever and erythemato-violaceous oedematous papules, plaques and nodules), laboratory (neutrophilia and increased inflammatory markers), and histological (dermal neutrophilic infiltrate without vasculitis) features. Its pathophysiology is poorly understood but there seems to be an auto-inflammatory component related to mutations in inflammasome genes. It has been subdivided into its classic form, malignancy-associated, and drug-induced, according to its aetiology.
View Article and Find Full Text PDFSynthesis of Diazacyclic and Triazacyclic Small-Molecule Libraries Using Vicinal Chiral Diamines Generated from Modified Short Peptides and Their Application for Drug Discovery.
Pharmaceuticals (Basel)
November 2024
Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.
Small-molecule probes are powerful tools for studying biological systems and can serve as lead compounds for developing new therapeutics. Especially, nitrogen heterocycles are of considerable importance in the pharmaceutical field. These compounds are found in numerous bioactive structures.
View Article and Find Full Text PDFTowards Novel Antiplasmodial Agents-Design, Synthesis and Antimalarial Activity of Second-Generation β-Carboline/Chloroquine Hybrids.
Molecules
December 2024
Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, 10000 Zagreb, Croatia.
As the resistance of to the existing antimalarials increases, there is a crucial need to expand the antimalarial drug pipeline. We recently identified potent antimalarial compounds, namely harmiquins, hybrids derived from the β-carboline alkaloid harmine and 4-amino-7-chloroquinoline, a key structural motif of chloroquine (CQ). To further explore the structure-activity relationship, we synthesised 13 novel hybrid compounds at the position -9 of the β-carboline ring and evaluated their efficacy in vitro against 3D7 and Dd2 strains (CQ sensitive and multi-drug resistant, respectively).
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