In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2022.128783 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Fentanyl and Fentanyl Analog Screening Using ASAP-MS With LiveID Confirmation.
Rapid Commun Mass Spectrom
May 2025
Department of Chemistry, The University of North Texas, Denton, Texas, USA.
Rationale: Fentanyl and fentanyl analogs continue to pose a serious threat to the public health. The vast number of fentanyl analogs emerging on the black-market call for optimized analytical methods for the detection, analysis, and characterization of these extremely dangerous drugs.
Methods: Atmospheric pressure solids analysis probe (ASAP) mass spectrometry was used for the rapid analysis of 250 synthetic opioid standards, including 211 fentanyl analogs, 32 non-fentanyl related opioids, and 8 fentanyl precursors.
Untargeted Metabolomics and Bioactivities Assessment of Xylaria ellisii, an Endophytic Fungus Isolated from the Leaf of the Plant Acorus calamus Linn.
Curr Pharm Des
January 2025
Centre of Experimental Medicine and Surgery, Institute of Medical Sciences, Banaras Hindu University, Varanasi 221005, India.
Introduction: Fungal endophytes have mutualistic associations with the plant's host, communicating through genetic and metabolic processes. As a result, they gain the ability to generate therapeutically effective metabolites and their derivatives.
Methods: The current study aims to assess antioxidant potential along with the identification of robust metabolites within the crude extract of a potent endophytic fungus Xylaria ellisii isolated from leaf tissues of the Acorus calamus Linn plant.
Longitudinal omics data and preclinical treatment suggest the proteasome inhibitor carfilzomib as therapy for ibrutinib-resistant CLL.
Nat Commun
January 2025
Division of Molecular Genetics, German Cancer Research Center (DKFZ), Heidelberg, Germany.
Chronic lymphocytic leukemia is a malignant lymphoproliferative disorder for which primary or acquired drug resistance represents a major challenge. To investigate the underlying molecular mechanisms, we generate a mouse model of ibrutinib resistance, in which, after initial treatment response, relapse under therapy occurrs with an aggressive outgrowth of malignant cells, resembling observations in patients. A comparative analysis of exome, transcriptome and proteome of sorted leukemic murine cells during treatment and after relapse suggests alterations in the proteasome activity as a driver of ibrutinib resistance.
View Article and Find Full Text PDFSynthesis of a di-O-acylated deoxynojirimycin (DNJ) derivative and evaluation of its antibacterial and antibiofilm activity against Staphylococcus aureus and Stenotrophomonas maltophilia.
Carbohydr Res
January 2025
Department of Chemical Sciences, University of Naples Federico II, Naples, I-80126, Italy.
Herein we report the synthesis of a novel di-O-acylated DNJ derivative, conceived to study whether iminosugar derivatization with a lipophilic acyl moiety could positively affect its antibacterial properties. The well-known PS-TPP/I/ImH activating system was used to readily install the acyl chains on the iminosugar, leading to the desired compound in high yield. Biological assays revealed that a di-O-lauroyl DNJ derivative enhanced the antibacterial effect of gentamicin and amikacin against S.
View Article and Find Full Text PDFEnantioselective Decarboxylative Mannich Reactions of α,β-Unsaturated β'-Ketoacids and Isatin Imines: Application in the Synthesis of Spiro[indoline-3,2'-piperidine]-2,4'-diones.
Org Lett
January 2025
Department of Chemistry, Memorial University, St. John's, Newfoundland and Labrador A1B 3X7, Canada.
Organocatalytic, enantioselective decarboxylative Mannich reactions of α,β-unsaturated β'-ketoacids and isatin -Boc imines, to give the corresponding 3-carbamoyl-2-oxindole derivatives, were developed. Subsequent N-deprotection and diastereoselective, intramolecular, aza-Michael reaction of the free amine provides previously unreported spiro[indoline-3,2'-piperidine]-2,4'-diones.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!