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-β, β-β' trifused porphyrins: synthesis, spectral, electrochemical and DFT studies and their femtosecond third-order nonlinear optical properties.
Dalton Trans
January 2025
Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee, 247667, India.
-β, β-β' trifused porphyrins incorporating two distinct active methylene groups (MN = malononitrile and IND = 1,3-indanedione) and their corresponding metal complexes with Cu(II) and Zn(II) have been synthesized with good to excellent yields and characterized by various spectroscopic techniques and spectrometric methods. Single crystal X-ray analysis of the Zn(II) complex ZnTFPMB(MN) (where TFP = trifused porphyrin and MB = mono benzo) revealed a nonplanar 'armchair' type conformation with a twist angle of 24.10°.
View Article and Find Full Text PDFAn orally available P1'-5-fluorinated M inhibitor blocks SARS-CoV-2 replication without booster and exhibits high genetic barrier.
PNAS Nexus
January 2025
Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.
We identified a 5-fluoro-benzothiazole-containing small molecule, TKB272, through fluorine-scanning of the benzothiazole moiety, which more potently inhibits the enzymatic activity of SARS-CoV-2's main protease (M) and more effectively blocks the infectivity and replication of all SARS-CoV-2 strains examined including Omicron variants such as SARS-CoV-2 and SARS-CoV-2 than two M inhibitors: nirmatrelvir and ensitrelvir. Notably, the administration of ritonavir-boosted nirmatrelvir and ensitrelvir causes drug-drug interactions warranting cautions due to their CYP3A4 inhibition, thereby limiting their clinical utility. When orally administered, TKB272 blocked SARS-CoV-2 replication without ritonavir in B6.
View Article and Find Full Text PDFAntimicrobial polyketides from the endophytic fungus Fusarium asiaticum QA-6 derived from medicinal plant Artemisia argyi.
Phytochemistry
January 2025
CAS and Shandong Province Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, And Laboratory for Marine Biology and Biotechnology, Qingdao Marine Science and Technology Center, Nanhai Road 7, Qingdao, 266071, PR China; University of Chinese Academy of Sciences, Yuquan Road 19A, Beijing, 100049, PR China; Center for Ocean Mega-Science, Chinese Academy of Sciences, Nanhai Road 7, Qingdao, 266071, PR China. Electronic address:
Seven previously undescribed polyketide derivatives, fusariumtides A-G (1-7), together with three known analogues (8-10), were isolated from the culture extract of Fusarium asiaticum QA-6, an endophytic fungus obtained from the fresh stem tissue of the medicinal plant Artemisia argyi H. Lev. & Vaniot.
View Article and Find Full Text PDFAntibacterial activity of withanolides, labdane glucosides, flavonoids and other constituents from two populations of Physalis patula.
Fitoterapia
January 2025
Facultad de Ciencias Naturales, Universidad Autónoma de Querétaro, Col. Juriquilla 76230, Querétaro, Qro., Mexico. Electronic address:
Two populations of Physalis patula Miller collected in different localities (Querétaro and Teotihuacán) of Central México were analyzed. Eight new compounds including three withanolides, physapatolides A-C (1-3), two labdanes, 12-epi-physacoztomatin (10) and physapatulone (12), besides three 12-O-glucosyl labdanes, patulosides A-C (13-15), were isolated from these collections. A series of known withanolides, flavonoids, labdanes, sucrose esters, and sterols were also isolated.
View Article and Find Full Text PDFCopper inactivates DcsB by oxidizing the metal ligand Cys86 to sulfinic acid.
FEBS J
December 2024
Faculty of Pharmacy, Yasuda Women's University, Hiroshima, Japan.
N-hydroxy-l-arginine amidinohydrolase (EC:3.5.3.
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