- Translation of Mycobacterium Survival Strategy to Develop a Lipo-peptide based Fusion Inhibitor**
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The entry of enveloped virus requires the fusion of viral and host cell membranes. An effective fusion inhibitor aiming at impeding such membrane fusion may emerge as a broad-spectrum antiviral agent against a wide range of viral infections. Mycobacterium survives inside the phagosome by inhibiting phagosome–lysosome fusion with the help of a coat protein coronin 1. Structural analysis of coronin 1 and other WD40-repeat protein suggest that the trp-asp (WD) sequence is placed at distorted β-meander motif (more exposed) in coronin 1. The unique structural feature of coronin 1 was explored to identify a simple lipo-peptide sequence (myr-WD), which effectively inhibits membrane fusion by modulating the interfacial order, water penetration, and surface potential. The mycobacterium inspired lipo-dipeptide was successfully tested to combat type 1 influenza virus (H1N1) and murine coronavirus infections as a potential broad-spectrum antiviral agent.
- Sardar, Avijit,Lahiri, Aritraa,Kamble, Mithila,Mallick, Amirul I.,Tarafdar, Pradip K.
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supporting information
p. 6101 - 6106
(2021/02/01)
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- L-proline/cholesterol and diosgenin based thiourea cooperative system for the direct asymmetric aldol reaction in the presence of water
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A series of cholesterol and based hydrophobic urea and thiourea compounds were synthesized and successfully used as a cocatalyst for L-proline catalyzed aldol reactions in the presence of water. The anticonfigured products were obtained with good yields (up to 94%), high diastereoselectivities (up to 95:5), and high enantiomeric excesses (up to 93% ee). The successful results for catalytic efficiency of L-proline in the presence of water reveal the importance of the hydrophobic nature of cholesterol and diosgenin parts of thiourea on the reactivity and selectivity in the presence of water.
- Eymur, Serkan,Ta?ci, Enis,Uyanik, Arzu,Yilmaz, Mustafa
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p. 1278 - 1284
(2020/11/20)
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- Perylen-3-ylmethyl: Fluorescent photoremovable protecting group (FPRPG) for carboxylic acids and alcohols
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Perylen-3-ylmethyl demonstrated as a new fluorescent photoremovable protecting group (FPRPG) for carboxylic acids and alcohols. Carboxylic acids including amino acids were protected as their corresponding esters by coupling with FPRPG, perylen-3-ylmethyl. Photophysical studies of caged esters showed that they all exhibited strong fluorescence properties and their fluorescence quantum yields were in the range of 0.85-0.95. Irradiation of the caged esters using visible light (≥410 nm) in aqueous acetonitrile released the corresponding carboxylic acids in high chemical (94-97%) and quantum (0.072-0.093) yields. The results obtained from the photolysis of the caged ester in different solvents indicated that solvent has influence on the rate of photorelease. Further, we also explored the ability of FPRPG, perylen-3-ylmethyl for the protection of alcohols and phenols.
- Jana, Avijit,Ikbal, Mohammed,Singh, N.D. Pradeep
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scheme or table
p. 1128 - 1136
(2012/02/16)
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- 1-(Hydroxyacetyl)pyrene a new fluorescent phototrigger for cell imaging and caging of alcohols, phenol and adenosine
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1-(Hydroxyacetyl)pyrene has been introduced as a new fluorescent phototrigger for alcohols and phenols. Alcohols and phenols were protected as their corresponding carbonate esters by coupling with fluorescent phototrigger, 1-(hydroxyacetyl)pyrene. Photophysical studies of caged carbonates showed that they all exhibited strong fluorescence properties. Irradiation of the caged carbonates by visible light (≥410 nm) in aqueous acetonitrile released the corresponding alcohols or phenols in high chemical (95-97%) and quantum (0.17-0.21) yields. The mechanism for the photorelease was proposed based on Stern-Volmer quenching experiments and solvent effect studies. Importantly, 1-(hydroxyacetyl)pyrene showed as a phototrigger for rapid photorelease of the biologically active molecule adenosine. In vitro biological studies revealed that 1-(hydroxyacetyl)pyrene has good biocompatibility, cellular uptake property and cell imaging ability. The Royal Society of Chemistry and Owner Societies 2012.
- Jana, Avijit,Saha, Biswajit,Ikbal, Mohammed,Ghosh, Sudip Kumar,Singh, N. D. Pradeep
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p. 1558 - 1566
(2013/02/26)
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- WATER-SOLUBLE POLYSACCHARIDE ETHERS AND THEIR USE
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The invention relates to modified polysaccharide ethers having a weight-averaged molecular weight of 40000 to 50000 g/mole, zero shear viscosity of more than 10 Pas, and pseudoplasticity of more than 20, obtainable by reacting cellulose-based polysaccharide ether(s) with at least one mesogenic modification agent or modified polysaccharide ethers, obtainable by reacting polysaccharide ether(s) selected from the group consisting of hydroxypropylmethyl cellulose (HPMC), hydroxyethylmethyl cellulose (HEMC), methyl cellulose, and cellulose ethers with methyl and/or ethyl and/or propyl groups and mixtures thereof, with at least one mesogenic modification agent. Said substances can be used to produce gel-like to stable aqueous preparations having viscoelastic flow properties, which are suited for use in the human body, particularly within the scope of ophthalmologic procedures.
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- Method for the preparation of aliphatic chloroformates
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A method for preparing an aliphatic chloroformate comprising, introducing a mixture of at least one aliphatic hydroxyl compound, phosgene, at least one solvent, and optionally at least one organic base into a flow reactor to obtain a unidirectional flowing reaction mixture. The at least one aliphatic hydroxyl compound comprises at least one aliphatic hydroxyl group. The unidirectional flowing reaction mixture is maintained at a temperature between about 0° C. and about 60° C. to produce a single product stream comprising an aliphatic chloroformate.
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Page/Page column 7-8
(2008/06/13)
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- A multiple switching bisthienylethene and its photochromic fluorescent organogelator
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A multiple switching fluorescent photochromic bisthienylethene bridged naphthalimide bearing cholesteryl groups was synthesized and its organogelator showed excellent photo-responsive and thermal reversible performance by light, thermal. The Royal Society of Chemistry 2006.
- Wang, Sheng,Shen, Wei,Feng, Yanli,Tian, He
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p. 1497 - 1499
(2008/02/11)
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- Methods and articles for the delivery of therapeutic agents
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Articles and methods for the delivery of drugs and/or nucleic acids. Articles including a nanoparticle are provided that may be used for the delivery of a drug, a nucleic acid, or both, to a subject. The articles may be of polymeric material and may self-assemble.
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- CARBOXYLIC-ACID-ESTER-TYPE TETRAALKYL AMMONIUM SALTS, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS
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The invention relates to novel carboxylic-acid-ester-type tetraalkyl ammonium salts, the production thereof and the pharmaceutical use thereof in fungal and bacterial infections and as potential inhibitors in the biosynthesis of cholesterol. The compounds, which are produced by reacting aliphatic or phenolic alcohol functions with active chlorocarboxylic acid esters and amines, can contain one or several of said ammonium salts on a carrier molecule comprising a system of anellated rings or long-chained hydrocarbons. Said compounds are characterised by high and specific activity against Candida species, particularly when steroids are used as carriers.
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Page/Page column 7
(2008/06/13)
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- GENE CARRIERS WITH THE USE OF POLYSACCHARIDE AND PROCESS FOR PRODUCING THE SAME
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Disclosed are gene carriers utilizing β-1,3-glucan and methods of preparing the same. The β-1,3-glucan has at least one 1,6-glucopyranoside branch and is chemically modified through periodate oxidation and reductive animation so as to impart nucleic acid-binding functional groups (for example, cationic functional groups) to at least some of the 1,6-glucopyranoside branches thereof. Triple helix β-1,3-glucan is dissolved in a polar organic solvent to form single-stranded β-1,3-glucan. By replacing, in the presence of a nucleic acid, the polar organic solvent for the solution containing the chemically modified single-stranded β-1,3-glucan by water, a complex (gene carrier) is formed in which the nucleic acid is bound to double-stranded β-1,3-glucan.
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- Synthesis of cholesterol derivatives. II1 Carbamates derivatlves of heterocycle compounds
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Carbamates derivatives from cholesterol, similarly carbonates benzoates, are compounds with liquid crystals properties. Cholesteryl carbamates were prepared by the reactions of cholesteryl chloroformate with amine derivatives of heterocyclic compounds, in the prersence of pyridine as an acid acceptor. A new crown coupound with two cholesteryl side arms was synthesised and its transport properties were studied. The compounds were characterised by IR and NMR measurements. The texture of the mesophase was determined with a polarising microscope equipped with a hot stage.
- Baciu, Ion,C?rlanaru, Carmen,Ionitǎ, Gabriela,Drǎghici, Constantin
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p. 633 - 636
(2007/10/03)
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- (Aryltelluro)formates as precursors of alkyl radicals: Thermolysis and photolysis of primary and secondary alkyl (aryltelluro)formates
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Alkyl (aryltelluro)formates are effective precursors of oxyacyl, methyl, and primary and secondary alkyl radicals. At room temperature, irradiation of a benzene solution of methyl (aryltelluro)-formates 10-12, 2-methylpropyl (aryltelluro)formates 14 and 15, octyl (phenyltelluro)formate (17), cyclohexyl (aryltelluro)formates 19 and 20, 3β-cholestanyl (aryltelluro)formates 22 and 23, cholesteryl (phenyltelluro)formate (24) and benzyl (phenyltelluro)formate (27) with a 250-W low-pressure mercury lamp leads to the formation of oxyacyl radicals (34), which can be trapped by diphenyl diselenide to give the corresponding alkyl (phenylseleno)formates 13, 16, 18, 21, 24, 26, and 28 with excellent overall conversions. Thermolysis of these telluroformates at 160 °C in the dark leads to the formation of methyl and primary and secondary alkyl aryl tellurides 36-43 in excellent yields. Presumably, these transformations involve oxyacyl radicals, which undergo subsequent decarboxylation at the elevated temperature to afford alkyl radicals, which become involved in further radical chemistry. When 1-(benzylseleno)-5-hexyl (phenyltelluro)formate (44) was thermolysed under these conditions, 2-methylselenane (45) was observed as the sole selenium-containing product, demonstrating the synthetic utility of (aryltelluro)formates as alkyl radical precursors.
- Lucas, Mathew A.,Schiesser, Carl H.
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p. 5754 - 5761
(2007/10/03)
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- Structure-Activity Relationships of Cytotoxic Cholesterol-Modified DNA Duplexes
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Short DNA duplexes with cholesterol linked at the 3'-terminus of each strand have unique, selective cytotoxic properties.The structural requirements for biological activity were explored through chemical synthesis of analogs and testing in cultured hepatoma cells.Effects of modifications to the sequence, backbone, 3'-sterol, 3;-linker, and 5'-terminus were evaluated.Self-complementary 3'-modified oligodeoxynucleotide (ODN) 10-mers were prepared from solid supports bearing the modification and linker of interest.Any changes to the normal phosphodiester backbone were poorly tolerated.The presence of cholesterol or a closely related sterol was an absolute requirement for activity.The length and position of attachment of the linker to cholesterol was important, with longer linkers showing reduced activity.Large, lipophilic groups at the 5'terminus gave reduced cytotoxicity and poor solubility properties.The short length and unique structure of these ODNs allowed efficient automated synthesis on a 400 μmol scale and simplified purification.
- Reed, Michael W.,Lukhtanov, Eugeny A.,Gorn, Vladimir V.,Lucas, Deborah D.,Zhou, James H.,et al.
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p. 4587 - 4596
(2007/10/03)
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- SYNTHESIS AND UV SPECTRAL STUDIES OF 3 β-CHOLESTERYL-(SUBSTITUTED)PHENYL CARBONATE DERIVATIVES
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Twenty-eight 3β-cholesteryl-(substituted)phenyl carbonates (phenyl substituents: CH3, F, Cl, Br, I, CN, CHO, NO2 and COOC2H5, in ortho, meta and para positions) were synthesized; their UV spectra are interpreted as perturbed benzene spectra.
- Csaszar, Jozsef,Agocs, Pal Mihaly
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p. 313 - 318
(2007/10/02)
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- PREPARATION AND UV SPECTRAL STUDIES OF 4-(3β-CHOLESTERYLOXYCARBONYLOXY)-BENZYLIDENE-4'-ACETAMINOANILINE
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4-(3β-Cholesteryloxycarbonyloxy)-benzylidene-4'-acetaminoaniline with liquid crystal properties was prepared in two different ways.The UV spectra of the above molecule and of the intermediate Schiff base were studied.
- Agocs, Pal Mihaly,Csaszar, Jozsef
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p. 541 - 546
(2007/10/02)
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