We synthesized bicyclic ether sialidase inhibitors such as tetrahydro-furan-2-yl, tetrahydro-pyran-2-yl, and oxepan-2-yl derivatives related to zanamivir. These compounds substituted by diol at the C-3' and C-4' positions resulted in the retention of low nanomolar inhibitory activities against not only influenza A virus sialidase but also influenza A virus in cell culture. Compound 11a in particular showed comparable efficacy in vivo relative to that of oseltamivir phosphate.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(02)01039-9 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Ramifloraolides A - D, four highly oxygenated picrotoxane-type sesquiterpenoids from the stems of Baccaurea ramiflora and their antithrombotic activity.
Bioorg Chem
November 2024
Center for Pharmaceutical Sciences, Faculty of Life Science and Technology, Kunming University of Science and Technology, Chenggong Campus, Kunming 650500, PR China. Electronic address:
A phytochemical investigation of the ethanol extract from air-dried stems of Baccaurea ramiflora led to the isolation of four highly oxygenated picrotoxane-type sesquiterpenoids, ramifloraolides A - D (1-4). Their structures were elucidated by comprehensive spectroscopic data (HRESIMS, IR, 1D, and 2D NMR), and their absolute configuration of them were unambiguously determined by single-crystal X-ray diffraction. Structurally, all compounds possess a unique [4.
View Article and Find Full Text PDFScreening of lipase TiL from Tilletia indica for chemo-enzymatic epoxidation of alkenes.
Enzyme Microb Technol
February 2025
Laboratory of Biocatalysis and Synthetic Biotechnology, State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China.
Lipase can mediate the chemo-enzymatic epoxidation of alkenes with the presence of free carboxylic acid and hydrogen peroxide. Four novel lipases with the abilities of chemo-enzymatic epoxidation were mined from the gene database. Lipase TiL originated from Tilletia indica was identified with significant activity on formation of methyl epoxystearate from methyl oleate.
View Article and Find Full Text PDFTen-Step Total Synthesis of (±)-Phaeocaulisin A Enabled by Cyclopropanol Ring-Opening Carbonylation.
J Am Chem Soc
November 2024
Department of Chemistry, Emory University, Atlanta, Georgia 30322, United States.
We report an efficient total synthesis of (±)-phaeocaulisin A, a guaianolide sesquiterpene natural product possessing a complex tetracyclic skeleton embedded with an oxaspirolactone and a fused bicyclic lactone, four oxygen-containing stereocenters, and an 8-oxabicyclo[3.2.1]octane core.
View Article and Find Full Text PDFData mining of PubChem bioassay records reveals diverse OXPHOS inhibitory chemotypes as potential therapeutic agents against ovarian cancer.
J Cheminform
October 2024
University of Wisconsin-Madison, UW-Carbone Cancer Center, Drug Development Core, Small Molecule Screening Facility, Wisconsin Institutes for Medical Research, 1111 Highland Avenue, Madison, WI, 53705, USA.
Focused screening on target-prioritized compound sets can be an efficient alternative to high throughput screening (HTS). For most biomolecular targets, compound prioritization models depend on prior screening data or a target structure. For phenotypic or multi-protein pathway targets, it may not be clear which public assay records provide relevant data.
View Article and Find Full Text PDFCyclic ether and anhydride ring opening copolymerisation delivering new ABB sequences in poly(ester--ethers).
Chem Sci
July 2024
Department of Chemistry, Chemistry Research Laboratory 12 Mansfield Road Oxford OX1 3TA UK
Poly(ester--ethers) are interesting as they combine the ester linkage rigidity and potential for hydrolysis with ether linkage flexibility. This work describes a generally applicable route to their synthesis applying commercial monomers and yielding poly(ester--ethers) with variable compositions and structures. The ring-opening copolymerisation of anhydrides (A), epoxides (B) and cyclic ethers (C), using a Zr(iv) catalyst, produces either ABB or ABC type poly(ester--ethers).
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!