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Investigation of small molecules disrupting dengue virus assembly by inhibiting capsid protein and blocking RNA encapsulation.
Mol Divers
September 2024
Saveetha Medical College and Hospitals, Center for Global Health Research, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, India.
Dengue fever is a significant global public health concern, causing substantial morbidity and mortality worldwide. The disease can manifest in various forms, from mild fever to potentially life-threatening complications. Developing effective treatments remains a critical challenge to healthcare systems.
View Article and Find Full Text PDFHybrid derivatives containing dimethyl fumarate and benzothiazole scaffolds for the potential treatment of multiple sclerosis; in silico & in vivo study.
Daru
December 2024
Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R., Iran.
Background: Multiple Sclerosis (MS) is a chronic autoimmune, inflammatory neurological disease of the CNS. Riluzole and dimethyl fumarate (DMF) are two FDA-approved drugs to treat amyotrophic lateral sclerosis (ALS) and MS. Riluzole (a benzothiazole derivative) inhibits glutamate release from nerve terminals by antagonizing the N-Methyl-D-Aspartate (NMDA) receptor, and DMF upregulates anti-oxidative pathways.
View Article and Find Full Text PDFQuinolone bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists.
Arch Pharm (Weinheim)
September 2024
Institut für Pharmazeutische und Medizinische Chemie, Universität Münster, Münster, Germany.
Cyclopenta[g]quinolones of type 4 were designed with the aim to bioisosterically replace the phenol of potent GluN2B ligands such as ifenprodil and Ro 25-6981 by the quinolone system and to restrict the conformational flexibility of the aminopropanol substructure in a cyclopentane system. The designed ligands were synthesized in an eight-step sequence starting with terephthalaldehyde (5). Key steps pf the synthesis were the intramolecular Friedel-Crafts acylation of propionic acids 10 to yield the cyclopenta[g]quinolinediones 11 and the Mannich reaction of diketone 11a followed by conjugate addition at the α,β-unsaturated ketone 12a.
View Article and Find Full Text PDFDesign, Synthesis, and Biological Evaluation of Derivatives as Novel Brain-Penetrant and Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
J Med Chem
March 2024
Hefei Institute of Pharmaceutical Industry Company, Ltd., Hefei 230088, China.
A series of structurally novel GluN2B NMDAR antagonists were designed, synthesized, and biologically evaluated as anti-stroke therapeutics by optimizing the chemical structure of , the active ingredient of traditional Chinese medicine identified via screening. The systematic structure-activity relationship study led to the discovery of with promising NMDAR-GluN2B binding affinity and antagonistic activity. Of the two enantiomers, exhibited significant inhibition (IC = 74.
View Article and Find Full Text PDFIndazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
J Med Chem
August 2023
Institut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, D-48149 Münster, Germany.
Negative allosteric modulation of GluN2B subunit-containing NMDA receptors prevents overstimulation, resulting in neuroprotective effects. Since the phenol of prominent negative allosteric modulators is prone to rapid glucuronidation, its bioisosteric replacement by an indazole was envisaged. The key step in the synthesis was a Sonogashira reaction of non-protected iodoindazoles with propargylpiperidine derivatives.
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