79-37-8Relevant articles and documents
In silico design and pharmacological evaluation of conjugates of atenolol with modified saccharide for cardiovascular targeting
Kumbhar, Smita Tukaram,Patil, Shitalkumar Shivgonda,Bhatia, Manish Sudesh
, p. 261 - 271 (2021)
Amongst a wide range of biological macromolecules, saccharides exhibit the potential to be specifically recognized by cell-surface receptors and hence can be utilized as ligands in targeted drug delivery. The current study aims to use saccharides viz. Galactose, Pectin and Chitosan to improve targeting of Atenolol by oxalyl chloride mediated grafting. Conjugates were engineered by grafting Atenolol, a cardiovascular agent with the modified saccharide units. The conjugates were characterized by FTIR, DSC and 1H NMR study. Drug release analysis and cellular uptake study was carried out using H9c2 cell lines which represent that concentration of drug in cells treated with all atenolol-saccharide conjugates is enhanced by almost two-folds in comparison with cells treated with atenolol solution. Thus cell line study confers the evidence of selective cardiac delivery. No significant cytotoxicity was observed in case of all synthesized conjugates in the Brine shrimp lethality bioassay. Possible binding of the developed conjugates with the GLUT-4 receptors was assessed by in silico analysis using homology model developed by Swiss Model server. Hence it was concluded that the application of these conjugates with saccharides in selective cardiovascular drug delivery can be a promising approach to increase bioavailability, minimize drug loss by degradation and prevent harmful side effects by increasing specific cell targeting. Graphical abstract: [Figure not available: see fulltext.]
Preparation method of [alpha]-oxo-2-furanacetic acid
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Paragraph 0032-0033; 0042-0043; 0050-0051, (2021/05/01)
The invention belongs to the field of preparation of organic compounds, and particularly relates to a preparation method of [alpha]-oxo-2-furanacetic acid, which comprises the following steps: 1) preparing oxalic acid and an organic alkali solution, controlling the temperature to 5-10 DEG C, dropwisely adding a trichloromethyl carbonate solution into the oxalic acid and organic alkali solution, and keeping the temperature for 2-4 hours until the solid is completely dissolved to obtain a solution A; obtaining a first solution; 2) preparing a furan and Lewis acid solution, controlling the temperature to be 20-25 DEG C, then dropwise adding the first solution into the furan and Lewis acid solution, and carrying out heat preservation for 1-2 hours to obtain a second solution; and 3) quenching the second solution at 0-10 DEG C to obtain the [alpha]-oxo-2-furanacetic acid. The preparation method disclosed by the invention does not generate nitric oxide and composite salt, and is low in treatment difficulty, low in environmental harm, low in temperature required by the whole reaction, low in energy consumption, simple in reaction step and short in time consumption.
Citrate plasticizer and preparation method thereof
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Paragraph 0054; 0057, (2021/05/29)
The invention discloses a citrate plasticizer and a preparation method thereof. The preparation method comprises the following steps: firstly, carrying out reaction on citric acid and alcohol to prepare citric acid triester; acylating dianhydride to prepare carboxyl-containing triester citrate; carrying out acylating chlorination on the carboxyl-containing triester citrate, and then carrying out esterification reaction on the carboxyl-containing triester citrate and tri(2-hydroxyethyl) isocyanurate to prepare triester citrate containing isocyanurate; and finally, esterifying with fatty acyl chloride to obtain the modified citrate plasticizer. The preparation method is simple to operate, wide in raw material source and mild in reaction condition, and meets industrial production. The prepared triester citrate containing isocyanurate has a good plasticizing effect and excellent thermal stability, low-temperature flexibility, solvent extraction resistance, migration resistance and flame retardance, and can be widely applied to plastic rubber plasticizers.
BIFUNCTIONAL CYTOTOXIC AGENTS
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Page/Page column, (2015/08/04)
Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.
Sensor Comprising Resrufin Levulinate Having Sulfite Ion Selectivity and Method for Monitoring Sulfite Ion Using the Same
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, (2012/06/16)
The present invention relates to a sensor comprising a resorufin compound having sulfite ion selectivity and a method for detecting sulfite ions using the same. More specifically, the resorufin compound may have outstandingly increased fluorescence intensity by a deprotection reaction that a levulinyl group is cleaved with a sulfite ion to be used as a selective fluorescence sensor of turn-on type, and also represent a chromogenic change to detect sulfite ions by naked eye.
Thienopyridine and furopyridine kinase inhibitors
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, (2008/06/13)
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Isotopically coded affinity markers 3
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, (2008/06/13)
The invention concerns isotopically coded affinity markers (ICAT) for mass spectrometric analysis of proteins, and the preparation and use if said markers.
Inhibition of the complete set of mammalian secreted phospholipases A 2 by indole analogues: A structure-guided study
Smart, Brian P.,Pan, Ying H.,Weeks, Amanda K.,Bollinger, James G.,Bahnson, Brian J.,Gelb, Michael H.
, p. 1737 - 1749 (2007/10/03)
Structure-guided design was employed in a search for potent and selective inhibitors of mammalian secreted phospholipases A2 (sPLA 2s). Using the X-ray structures of human groups IIA and X sPLA 2s (hGIIA and hGX) as templates, homology structural models were made for the other human and mouse sPLA2s (hGIB, mGIB, mGIIA, mGIIC, hGIID, mGIID, hGIIE, mGIIE, hGIIF, mGIIF, hGV, mGV, and mGX). Me-Indoxam is a previously discovered indole analogue that binds tightly to many sPLA 2s, and the X-ray structure of the hGX-Me-Indoxam complex was determined at a resolution of 2.0 A. Modeling suggests that the residues near the N1-substituent of Me-Indoxam vary significantly among the mammalian sPLA2s, and therefore a library of 83 N1- variants was prepared by parallel synthesis. Several Me-Indoxam analogues bearing a 4-(2-oxy-ethanoic acid) side chain were potent inhibitors (IC 50 5 μM) hGIID, mGIID, hGIIF, and mGIIF. Me-Indoxam analogues bearing a 5-(4-oxy-butanoic acid) side chain were generally less potent inhibitors. Although no compounds were found to be highly specific for a single human or mouse sPLA2, combinations of Me-Indoxam analogues were discovered that could be used to distinguish the action of various sPLA2s in cellular events. For example, Me-Indoxam and compound 5 are approximately 5-fold more potent on hGIIA than on hGV, and compound 21 is 10-fold more potent on hGV versus hGIIA.
Taxol enhancer compounds
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, (2008/06/13)
One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
Indole derivatives as anti-inflammatory agents
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, (2008/06/13)
This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents
