Quinolone is a privileged scaffold in medicinal chemistry and 4-Quinolone-3-Carboxamides have been reported to harbor vast therapeutic potential. However, conversion of N-1 substituted 4-Quinolone 3-Carboxylate to its corresponding carbamates is highly restrictive. This motivated us to adopt a much simpler, scalable and efficient methodology for the synthesis of highly pure N-1 substituted 4- Quinolone-3-Carboxamides with excellent yields. Our adopted methodology not only provides a robust pathway for the convenient synthesis of N-1 substituted 4- Quinolone-3-Carboxamides which can then be explored for their therapeutic potential, this may also be adaptable for the derivatization of other such less reactive carboxylate species.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9733071 | PMC |
http://dx.doi.org/10.1186/s13065-022-00902-1 | DOI Listing |
Nanomaterials (Basel)
December 2024
School of Power & Mechanical Engineering, Wuhan University, Wuhan 430072, China.
TiZrMoC coatings were deposited on Si(100) substrates using a DC dual magnetron sputtering. The composition was controlled by adjusting the sputtering parameters of the TiZrMo and graphite targets. The influence of graphite target current on the resulting coating properties was explored.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
December 2024
Westfälische Wilhelms-Universität Münster: Westfalische Wilhelms-Universitat Munster, Organisch-Chemisches Institut, Corrensstrasse 40, 48149, Münster, GERMANY.
Bicyclo[1.1.0]butanes (BCBs) have recently garnered significant research interest as versatile precursors for synthesizing potential [n.
View Article and Find Full Text PDFClin Infect Dis
December 2024
Division of Antivirals, Office of Infectious Diseases, Center for Drug Evaluation and Research, Food and Drug Administration, 10903 New Hampshire Ave, Silver Spring, Maryland 20993.
Background: PAXLOVID consists of nirmatrelvir, an inhibitor of SARS-CoV-2 main protease (Mpro), copackaged with ritonavir, a pharmacokinetic enhancer. Nirmatrelvir/ritonavir received emergency use authorization in the United States in 2021 and was approved in 2023. However, there is limited published information on SARS-CoV-2 clinical resistance to nirmatrelvir/ritonavir.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Department of Food Engineering, National Institute of Food Technology Entrepreneurship and Management, Kundli, India. Electronic address:
The present study investigates the effect of ultrasonication (US) amplitude (30 %, 50 %, and 70 %, time- 45 min) followed by octenyl succinic anhydride (OSA, 3 %) esterification on morphological, structural, functional, and rheological properties of sorghum starch. The increase in US amplitudes significantly (p < 0.05) increased the degree of substitution (DS) of esterified starch (0.
View Article and Find Full Text PDFJ Org Chem
December 2024
Medicinal Chemistry, Oncology R&D, AstraZeneca, The Discovery Centre, 1 Francis Crick Avenue, Cambridge CB2 0AA, United Kingdom.
The increasing popularity of the dihydrouracil motif in cereblon (CRBN) recruiting proteolysis-targeting chimeras (PROTACs) has necessitated the development of a facile, cost-effective, and high-yielding method for its introduction into molecules. To that end, we disclose herein an N-1 selective Pd-catalyzed cross-coupling of dihydrouracil with aryl electrophiles to provide access to medicinally relevant scaffolds in a single step. This approach exhibits excellent functional group tolerance and broad applicability to an abundance of (hetero)aryl halides and phenol derivatives and utilizes readily available catalyst/ligand systems.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!