Beilstein J Org Chem
December 2024
Methods for the preparation of 3-aryl-2-azirine-2,2-dicarboxylic acids and their amides, esters, and azides by FeCl-catalyzed isomerization of 3-aryl-5-chloroisoxazole-4-carbonyl chlorides into 3-aryl-2-azirine-2,2-dicarbonyl dichlorides followed by their reaction with nucleophiles are reported. Two approaches to the preparation of 3-aryl-5-chloroisoxazole-4-carbonyl chlorides have been developed.
View Article and Find Full Text PDFTo design a safe cellular system for testing inhibitors targeting the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, a genetic construct was engineered containing viral cDNA with two blocks of reporter genes while the genes encoding structural S, E, and M proteins were absent. The first reporter block, consisting of Renilla luciferase and green fluorescent protein (Rluc-GFP), was located upstream of the SARS-CoV-2 5'-UTR. Meanwhile, the second block represented by firefly luciferase and red fluorescent protein (Fluc-RFP) was positioned downstream of the transcription regulatory sequence (TRS-N).
View Article and Find Full Text PDF1,1-Di(alkoxycarbonyl)-4-cyclopentyl-2-azabuta-1,3-dienes react with DBU to form two types of heterocyclic products: 1-cyclopenta[]pyrid-1-ones and 3-hydroxy-1-pyrroles. These previously unobserved transformations proceed through the formation of 1-azapentadienyl anion which undergoes 1,6-shift of the alkoxycarbonyl group to the cyclopentyl moiety followed by 1,6-cyclization to form the cyclopentapyridone (path ) and 1,5-cyclization accompanied by 1,3-shift of the methoxy group followed by dialkyl carbonate elimination to afford the hydroxypyrrole (path ). The mechanisms of the reactions were studied using DFT calculations.
View Article and Find Full Text PDFWe have previously shown that 5-arylaminouracil derivatives can inhibit HIV-1, herpesviruses, mycobacteria, and other pathogens through various mechanisms. The purpose of this study was to evaluate the potential of 5-arylaminouracils and their derivatives against leukemia, neuroblastoma, and glial brain tumors. 5-Aminouracils with various substituents and their 5'-norcabocyclic and ribo derivatives were screened for cytotoxicity against two neuroblastoma cell lines (SH-SY5Y and IMR-32), K-562 lymphoblastic cells, HL-60 promyeoloblastic cells, and low-passage variants of well-differentiated glioblastoma multiforme (GBM5522 and GBM6138).
View Article and Find Full Text PDF-Heart rate variability (HRV) and photoplethysmographic waveform variability (PPGV) are available approaches for assessing the state of cardiovascular autonomic regulation. The goal of our study was to compare the frequency-domain features and low-frequency (LF) synchronization of the PPGV and HRV with increasing severity of cardiovascular diseases. -Our study included 998 electrocardiogram (ECG) and finger photoplethysmogram (PPG) recordings from subjects, classified into five categories: 53 recordings from healthy subjects, aged 28.
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