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Bioactive Sulfonamides Derived from Amino Acids: Their Synthesis and Pharmacological Activities.
Mini Rev Med Chem
January 2025
Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.
Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.
View Article and Find Full Text PDFA Stereocontrolled Synthesis of (+)-Febrifugine via Azide and Azide-Free Pathways.
Chem Asian J
January 2025
Kasetsart University - Bangkhen Campus: Kasetsart University, Chemistry, 50, Department of Chemistry, Faculty of Science, Kasetsart UNiversity, Ladyao, Chatu, 10900, Bangkok, THAILAND.
(+)-Febrifugine, a natural antimalarial compound with a promising therapeutic profile, has become a hot target for synthetic chemists seeking to optimize its biological activity and expand its therapeutic applications. In this research, we present a stereocontrolled synthesis of (+)-febrifugine using both azide and azide-free approaches. Starting from the commercially available chiral pool precursor, d-glucose, the synthesis was completed in 20 steps for both approaches.
View Article and Find Full Text PDFDiscovery and mechanism of a highly selective, antifungal acetyl CoA synthetase inhibitor.
Res Sq
January 2025
Department of Pediatrics, Carver College of Medicine, University of Iowa, Iowa City, IA 52242.
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 , we identified an isoxazole-based ACS inhibitor with antifungal activity and exquisite selectivity for the Acs1 relative to human ACSS2 as well as other fungal ACSs.
View Article and Find Full Text PDFEvaluation of In Vitro Inhibition of -Hematin Formation: A Step Towards a Comprehensive Understanding of the Mechanism of Action of New Arylamino Alcohols.
Microorganisms
December 2024
Agents Infectieux, Résistance et Chimiothérapie (AGIR), UR 4294, Université de Picardie Jules Verne, 1 rue des Louvels, 80037 Amiens, France.
Currently, artemisinin-based combination therapy is recommended as first-line treatment of uncomplicated malaria. Arylamino alcohols (AAAs) such as mefloquine (MQ) are the preferred partner drugs due to their longer half-life, reliable absorption and strong antimalarial activity. However, the mode of action of MQ remains poorly understood and its neurotoxicity limits its use.
View Article and Find Full Text PDFNovel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties.
Eur J Med Chem
February 2025
School of Pharmacy and Food Engineering, Wuyi University, 529020, Jiangmen, China; Department of Chemistry, University of Liverpool, L69 7ZD, Liverpool, UK. Electronic address:
Aryl quinolone derivatives can target the cytochrome bc complex of Plasmodium falciparum, exhibiting excellent in vitro and in vivo antimalarial activity. However, their clinical development has been hindered due to their poor aqueous solubility profiles. In this study, a series of bioisosteres containing saturated heterocycles fused to a 4-pyridone ring were designed to replace the inherently poorly soluble quinolone core in antimalarial quinolones with the aim to reduce π-π stacking interactions in the crystal packing solid state, and a synthetic route was developed to prepare these alternative core derivatives.
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