A5056155365- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Asymmetric Synthesis and Catalysis
- Biological Activity of Diterpenoids and Biflavonoids
- Crystallography and molecular interactions
- Chemical Synthesis and Analysis
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Reactions
- Influenza Virus Research Studies
- Natural product bioactivities and synthesis
- Radical Photochemical Reactions
- Coordination Chemistry and Organometallics
- Sulfur-Based Synthesis Techniques
- Oxidative Organic Chemistry Reactions
- Organic Chemistry Cycloaddition Reactions
- Glycosylation and Glycoproteins Research
- Synthetic Organic Chemistry Methods
- Synthesis and Biological Evaluation
- Fluorine in Organic Chemistry
- Molecular Sensors and Ion Detection
- Synthesis and Catalytic Reactions
- Phytochemistry and Biological Activities
- Synthesis and Reactions of Organic Compounds
- Synthesis of heterocyclic compounds
- Chemical Reaction Mechanisms
National Taiwan University
2015-2024
Tropical Crops Genetic Resources Institute
2022-2024
Genomics Research Center, Academia Sinica
2014-2023
Lear (United States)
2019
Genomics (United Kingdom)
2017
Academia Sinica
2002-2016
National Defense Medical Center
2004-2014
Johns Hopkins University
2011
Taipei Medical University
2007
Institute of Biological Chemistry, Academia Sinica
2004-2007
Severe acute respiratory syndrome (SARS) is an infectious disease caused by a novel human coronavirus. Currently, no effective antiviral agents exist against this type of virus. A cell-based assay, with SARS virus and Vero E6 cells, was developed to screen existing drugs, natural products, synthetic compounds identify anti-SARS agents. Of >10,000 tested, approximately 50 were found active at 10 microM; among these compounds, two are drugs (Reserpine 13 Aescin 5) several in clinical...
Using d-xylose as an appropriate chiral precursor, we have synthesized active neuraminidase inhibitor oseltamivir, antiflu drug Tamiflu, and novel phosphonate congeners that exhibit even stronger activities by inhibiting the neuraminidases of wild-type H274Y mutant H1N1 H5N1 viruses. Molecular modeling neuraminidase−phosphonate complex indicates a pertinent binding mode with three arginine residues in site. Discovery such potent inhibitors will offer opportunity to development new...
We have designed a low fluorescent azido-BODIPY-based probe AzBOCEt (Az10) that undergoes copper(I)-catalyzed 1,3-dipolar cycloadditions with alkynes to yield strongly triazole derivatives. The quantum of product T10 is enhanced by 52-fold as compared upon excitation at wavelength above 500 nm. Quantum mechanical calculations indicate the increase in fluorescence formation due lowering HOMO energy level aryl moiety reduce process acceptor photoinduced electron transfer. shown label...
Amyotrophic lateral sclerosis (ALS) associated with TAR DNA-binding protein 43 (TDP-43) aggregation has been considered as a lethal and progressive motor neuron disease. Recent studies have shown that both C-terminal TDP-43 (C-TDP-43) aggregates oligomers were neurotoxic pathologic agents in ALS frontotemporal lobar degeneration (FTLD). However, misfolding long an undruggable target by applying conventional inhibitors, agonists, or antagonists. To provide this unmet medical need, we aim to...
A variety of aldehydes reacted with iodine in ammonia water at room temperature to give the nitrile intermediates, which were trapped by addition hydrogen peroxide, sodium azide, or dicyandiamide produce their corresponding amides, tetrazoles, and 1,3,5-triazines modest high yields. The one-pot tandem reactions conducted media, products obtained simply extraction filtration.
The neutral receptor N,N'-bis{3,5-di[(1-pyrenylmethyl)carbamoyl]benzyl} pyridine-2,6-dicarbamide (2) provides a pseudo-tetrahedron cleft and multiple hydrogen bondings to form 1:1 complex with phosphate ion in highly selective manner, by comparison other anions (F-, Cl-, Br-, SCN-, AcO-, NO3-, ClO4-, HSO4-). binding strength can be inferred from the emission intensity ratio of pyrene monomer (λmax 377 nm) excimer 477 nm). Fluorescence titration, X-ray analysis, NMR studies support proposed...
A series of primary alcohols and aldehydes were treated with iodine in ammonia water under microwave irradiation to give the intermediate nitriles, which without isolation underwent [2 + 3] cycloadditions dicyandiamide sodium azide afford high yields corresponding triazines tetrazoles, including α-amino- dipeptidyl tetrazoles optical purity.
Tamiflu and the highly potent neuraminidase inhibitor tamiphosphor have been synthesized in 11 steps greater than 20 % overall yields from an haloarene (1S,2S)-cis-diol. The key transformations include a regio- stereoselective bromoamidation, palladium-catalyzed carbonylation or phosphonylation reaction (see scheme; tamiflu: A=CO2Et, B=NH3+H2PO4−, tamiphosphor: A=PO(ONH4)2, B=NH2).
Pyreno[2,1-b]pyrrole and its dimeric derivative display excellent selectivity sensitivity for detection of fluoride ion, in comparison with chloride, bromide, iodide, acetate, dihydrogen phosphate, hydrogen sulfate, perchlorate, nitrate, thiocyanate ions. The bonding both formation subsequent dissociation, provides remarkable colorimetric fluorescent changes the visible region that are advantageous real-time on-site application. Detailed NMR dynamic fluorescence spectroscopic analyses...
Two phosphonate compounds 1a (4-amino-1-phosphono-DANA) and 1b (phosphono-zanamivir) are synthesized shown more potent than zanamivir against the neuraminidases of avian human influenza viruses, including oseltamivir-resistant strains. For first time, practical synthesis these is realized by conversion sialic acid to peracetylated phosphono-DANA diethyl ester (5) as a key intermediate in three steps novel approach. In comparison with zanamivir, high affinity can be partly attributable strong...
Abstract Background The timely and accurate diagnosis of specific influenza virus strains is crucial to effective prophylaxis, vaccine preparation early antiviral therapy. detection A viruses mainly accomplished using polymerase chain reaction (PCR) techniques or antibody-based assays. In conjugation with the immunoassay utilizing monoclonal antibody, mass spectrometry an alternative identify proteins derived from a target virus. Taking advantage large surface area-to-volume ratio,...
A series of dual-action compounds were designed to target histone deacetylase (HDAC) and 3-hydroxy-3-methylglutaryl coenzyme reductase (HMGR) by having a hydroxamate group essential for chelation with the zinc ion in active site HDAC key structural elements statin binding both proteins. In our study, hydroxamic acids prepared fused strategy are most promising cancer treatments. These showed potent inhibitory activities against HDACs HMGR IC50 values nanomolar range. also effectively reduced...
Benzaldehydes and acetophenones bearing tethered carbonyl chains underwent the intramolecular phenyl–carbonyl coupling reactions, by mediation of samarium diiodide hexamethylphosphoramide, to afford xanthenes fused benzocarbocyclic compounds containing hydroxyl substituents.
A diversified library of peptide anilides was prepared, and their inhibition activities against the SARS-CoV 3CL protease were examined by a fluorogenic tetradecapeptide substrate. The most potent inhibitor is an anilide derived from 2-chloro-4-nitroaniline, l-phenylalanine 4-(dimethylamino)benzoic acid. This competitive with Ki = 0.03 μM. molecular docking experiment indicates that P1 residue this distant nucleophilic SH Cys145 in active site.
This study provides a practical method for production of the antibodies against malachite green (MG) and its primary metabolite leucomalachite (LMG). Two ELISA kits are constructed with MG LMG detection residual in fish muscle fishpond water. The limit is established at level 0.05 µg/L both LMG. Our show advantages good specificity, high sensitivity, convenience rapid screening residues. sample water, without extraction or prior preparation, directly assayed by kit. More then 80 samples can...
Abstract We report the encapsulation of quantum dots with biologically important β‐ N ‐acetylglucosamine (GlcNAc) in different ratios, together studies their specific/sensitive multivalent interactions lectins and sperm by fluorimetry, transmission electron microscopy, dynamic light scattering confocal imaging techniques, flow cytometry. These GlcNAc‐encapsulated (QDGLNs) specifically bind to wheat germ agglutinin, cause fluorescence quenching aggregation. Further QDGLNs mannose‐encapsulated...
The push−pull conjugated molecules 2,7-bis-(1H-pyrrol-2-yl)ethynyl-1,8-naphthyridine (BPN) and 2,7-bis(1H-indol-2-yl)ethynyl-1,8-naphthyridine (BIN) adopting daad relays of proton donors (d) acceptors (a) form multiple hydrogen-bonding complexes with various monosaccharides that possess complementary adda sequences. Although the free BPN emits blue light at λmax = 475 nm in CH2Cl2, its complexation octyl β-d-glucopyranoside gives green fluorescence 535 nm. excellent photophysical properties...