Substituted phenols as the starting materials were transformed into substituted chromanones by substitution reaction and cyclization reaction, and then 3-(hydroxymethylene)chroman-4-ones were synthesized from substituted chromanones by condensation reaction; at last, the target compounds were synthesized from 3-(hydroxymethylene)chroman-4-ones by chlorination reaction. Their structures were confirmed by 1H NMR and MS. The antifungal activity of the target compounds in vitro was measured by consecutive double dilution, and the result of antifungal experiment indicated that the target compounds had good antifungal action on most fungi tested in vitro. The MIC value of compounds 4c, 4e, 4g and 4h on M. gypseum is 1 microg x mL(-1), better than fluconazole and amphotericin B.
Download full-text PDF |
Source |
---|
Ann Hematol
January 2025
Service de Thérapie Cellulaire et d'Hématologie Clinique, CHU Estaing, Clermont-Ferrand, France.
The advent of BTK inhibitors has been transformative in the management of patients with chronic lymphocytic leukemia or other B-cell lymphoproliferative disorders. However, emergence of BTK or PLCG2 mutations lead to resistance to these compounds and are now a growing concern in clinical practice. Assessing BTK mutations is now becoming a priority to guide the therapeutic decision at further relapse.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Bio-System Pharmacology, Graduate School of Medicine, Osaka University, 2-2, Yamadaoka, Suita, Osaka, 565-0871, Japan.
L-type amino acid transporter 1 (LAT1, SLC7A5), overexpressed in various cancers, mediates the uptake of essential amino acids crucial for tumor growth. It has emerged as a promising target for cancer therapy. Nanvuranlat (JPH203/KYT-0353), a LAT1 inhibitor, has shown antitumor activity in preclinical studies and efficacy in biliary tract cancer during clinical trials.
View Article and Find Full Text PDFSci Rep
January 2025
Institute of Science and High Technology and Environmental Sciences, Graduate University of Advanced Technology, Kerman, Iran.
Co-pyrolysis is an efficient approach for municipal sewage sludge (SS) treatment, facilitating the production of biochar and promoting the stabilization and removal of heavy metals, particularly when combined with chlorinated materials. This study explores the impact of pyrolysis temperatures (400 °C and 600 °C) and chlorinated additives (polyvinyl chloride (PVC) as an organic chloride source and ferric chloride (FeCl) as an inorganic chloride source) at 10% and 20% concentrations, on the yield, chemical speciation, leachability, and ecological risks of arsenic (As), chromium (Cr), and zinc (Zn) in biochar derived from SS. The results revealed that increasing the pyrolysis temperature from 400 to 600 °C significantly reduced biochar yield due to enhanced volatilization of organic components, as well as the removal of heavy metals in interaction with chlorinated materials.
View Article and Find Full Text PDFJ Invest Dermatol
January 2025
Department of Cell Biology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan. Electronic address:
Contact hypersensitivity (CHS) and atopic dermatitis (AD) are pervasive inflammatory skin diseases with similar symptoms, and the global prevalence of both conditions is steadily rising. Many compounds and biotics have been developed to target molecules critical to the etiology or pathogenesis of CHS and AD. However, such molecules are sometimes ineffective or lose potency over the therapeutic course.
View Article and Find Full Text PDFBioorg Chem
January 2025
Medicinal Chemistry Research Laboratory, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Campus-2, Ghatikia, Kalinga Nagar, Bhubaneswar, Odisha 751003, India. Electronic address:
Heterocyclic chemistry gathered a wide audience due to their presence in potential drug candidates and being attractive synthons initiating several retro-syntheses the organic as well as in medicinal chemistry fields. Among them, azetidinones have been a subject of discussion due to their serendipity, curiosity, versatility by Penicillin and Cephalosporins as β-lactam antibiotics. Despite possessing a large margin of biological activities, azetidinones mainly work as antimicrobial, interfering with bacterial cell-wall synthesis blocking transpeptidase.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!