A5100708416- Adenosine and Purinergic Signaling
- HIV/AIDS drug development and treatment
- Synthetic Organic Chemistry Methods
- Heme Oxygenase-1 and Carbon Monoxide
- Malaria Research and Control
- Pharmacological Receptor Mechanisms and Effects
- Receptor Mechanisms and Signaling
- Influenza Virus Research Studies
- Chemical Synthesis and Analysis
- Genomics, phytochemicals, and oxidative stress
- Synthesis of Organic Compounds
- Chemical synthesis and alkaloids
- Mosquito-borne diseases and control
- Click Chemistry and Applications
- Peptidase Inhibition and Analysis
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Biological Evaluation
- Signaling Pathways in Disease
- Natural product bioactivities and synthesis
- Asymmetric Synthesis and Catalysis
- Pharmacological Effects of Natural Compounds
- Sulfur Compounds in Biology
- Cancer Treatment and Pharmacology
- Fungal Plant Pathogen Control
- Oxidative Organic Chemistry Reactions
Wonkwang University
2012-2024
Ewha Womans University
2023
Korea Advanced Institute of Science and Technology
2022
Chosun University
2017-2022
Chosun University Hospital
2017
Hanyang University
2007
Korea Research Institute of Bioscience and Biotechnology
2006
Korea Atomic Energy Research Institute
2006
Sungkyunkwan University
2006
National Medical Center
2005
Field diagnostic tools for avian influenza (AI) are indispensable the prevention and controlled management of highly pathogenic AI-related diseases.More accurate, faster networked on-site monitoring is demanded to detect such AI viruses with high sensitivity as well maintain up-to-date information about their geographical transmission.In this work, we assessed clinical field-level performance a smartphone-based fluorescent device an efficient reflective light collection module using...
Preference for the northern (N) ring conformation of ribose moiety adenine nucleotide 3',5'-bisphosphate antagonists P2Y(1) receptors was established by using a ring-constrained methanocarba (a bicyclo[3.1.0]hexane) as substitute (Nandanan et al. J. Med. Chem. 2000, 43, 829-842). We have now combined (N)-methanocarba modification with other functionalities at 2-position moiety. A new synthetic route to this series bisphosphate derivatives introduced, consisting phosphorylation pseudoribose...
2-Chloro-<i>N</i><sup>6</sup>-methyl-(<i>N </i>)-methanocarba-2′-deoxyadenosine-3′,5′- bisphosphate (MRS2279) was developed previously as a selective high-affinity, non-nucleotide P2Y<sub>1</sub> receptor (P2Y1-R) antagonist (<i>J Med Chem</i><b>43:</b>829–842, 2002; <i>Br J Pharmacol</i><b>135:</b>2004–2010, 2002). We have taken advantage of the<i>N</i><sup>6</sup>-methyl substitution in the adenine base to incorporate [<sup>3</sup>H]methylamine into synthesis [<sup>3</sup>H]MRS2279 high...
The potency of nucleotide antagonists at P2Y1 receptors was enhanced by replacing the ribose moiety with a constrained carbocyclic ring (Nandanan, et al. J. Med. Chem. 2000, 43, 829−842). We have now synthesized ring-constrained methanocarba analogues (in which fused cyclopropane constrains pseudosugar ring) adenine and uracil nucleotides, endogenous activators P2Y receptors. Methanocarba-adenosine 5'-triphosphate (ATP) fixed in either Northern (N) or Southern (S) conformation, as defined...
Activation by ADP of both P2Y1 and P2Y12 receptors in platelets contributes to platelet aggregation, antagonists at these receptor subtypes have antithrombotic properties. In an earlier publication, we characterized the SAR as acyclic analogues adenine nucleotides, containing two phosphate groups on a symmetrically branched aliphatic chain, attached 9-position adenine. this study, focused antiaggregatory effects P2Y related 2-chloro-N6-methyladenine-9-(2-methylpropyl) scaffold, uncharged...
Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione] induces heme oxygenase-1 (HO-1) expression via activation of the nuclear factor-erythroid-2-related factor 2 (Nrf2), whereas tetrahydrocurcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-3,5-heptanedione], one curcumin in vivo metabolites, has no effect on HO-1 and Nrf2 activation. The aim this study was to investigate whether dimethoxycurcumin [1,7-bis(4,3-dimethoxyphenyl)-1,6-heptadiene-3,5-dione], a synthetic analogue with...
In the search for improved selective antagonist ligands of A2B adenosine receptor, which have potential as antiasthmatic or antidiabetic drugs, we synthesized and screened a variety alkylxanthine derivatives substituted at 1-, 3-, 7-, 8-positions. Competition 125I-ABOPX (125I-3-(4-amino-3-iodobenzyl)-8-(phenyl-4-oxyacetate)-1-propylxanthine) binding in membranes stably transfected HEK-293 cells revealed uniformly higher affinity (<10-fold) these xanthines human than rat receptors. Binding to...
The activation of P2Y1 receptors in platelets contributes to platelet aggregation, and selective antagonists are sought as potential antithrombotic agents. We reported (Kim et al. J. Med. Chem. 2000, 43, 746−755) that acyclic analogues adenine nucleotides, containing two phosphate groups on a symmetrically branched aliphatic chain, attached at the 9-position adenine, moderately potent receptor antagonists. In this study we have varied chain structure, include asymmetric substitution,...
Preference for the Northern (N) ring conformation of ribose moiety nucleotide 5'-triphosphate agonists at P2Y1, P2Y2, P2Y4, and P2Y11 receptors, but not P2Y6 was established using a ring-constrained methanocarba (a 3.1.0-bicyclohexane) as substitute (Kim et al. J. Med. Chem. 2002, 45, 208−218.). We have now combined (N)-methanocarba modification adenine nucleotides with other functionalities known to enhance potency P2 receptors. The newly synthesized analogues determined in stimulation...
The widespread emergence of anti-malarial drug resistance has necessitated the discovery novel candidates. In this study, chloroquine derivatives were evaluated for improved activity.Novel two (SKM13 and SKM14) synthesized based on (CQ) template containing modified side chains such as α,β-unsaturated amides phenylmethyl group. selective index indicated that SKM13 was 1.28-fold more effective than CQ against CQ-resistant strain Plasmodium falciparum. An in vivo mouse study demonstrated (20...
The synthesis and biological evaluation of a bicyclo[3.1.0]hexene nucleoside designed as conformational mimic the anti-HIV agent stavudine (1, D4T) is described. unsaturated methanocarbocyclic pseudosugar N-MCD4T (2) was constructed from an iodo-substituted precursor by DBU-catalyzed olefination reaction. Mitsunobu coupling with N(3)-benzoylthymine afforded desired target after deprotection. Both D4T are in North (N) hemisphere pseudorotational cycle but 70 degrees away perfect N (P = 0 )...
Great efforts have been made to develop robust signal-generating fluorescence materials which will help in improving the rapid diagnostic test (RDT) terms of sensitivity and quantification. In this study, we developed coumarin-derived dendrimer-based fluorescent immunochromatographic strip (FICT) assay with enhanced as a quantitative tool typical RDT environments. The accuracy proposed FICT was compared that dot blot immunoassay techniques conventional RDTs. Through conjugation dendrimers...
The tandem Diels-Alder reaction leads to a highly stereoselective two-step synthesis of taxane nucleus from two readily available acyclic precursors in 50% overall yield.
Since ionic liquids (ILs), salts with a melting point below 100 °C, have unique physicochemical properties, they been spotlighted as novel alternatives to organic solvents. However, studies relating polymorph control using IL solvent not yet performed due the numerous (1018) available types unknown effects on of polymorphic transformation, and extremely high unit price compared conventional Presently, pharmaceutical industry highly prefers soluble form-I among several polymorphs active...