- Liposome Enhanced Detection of Amyloid Protein Aggregates
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Thioflavin-T is used to image amyloid aggregates because of the excellent turn-on fluorescence properties, but binding affinities are low. By mounting multiple dye units on the surface of a vesicle, the binding affinity for α-synuclein fibrils is increased by three orders of magnitude, and the optical response is increased. Cooperative interactions of the dye headgroup and lipid with the protein provide a general strategy for the construction of multivalent amyloid probes based on vesicles.
- Kocsis, Istvan,Sanna, Elena,Hunter, Christopher A.
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- Synthesis of alkyl [(alkyl 6-deoxy-alpha-D-gluco-heptopyranosyl- uronate) 6-deoxy-alpha-D-gluco-heptopyranosid]uronates, a novel type of mirror pseudo cord factor.
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The 1-octyl, 1-pentadecyl, 1-hexadecyl, 1-heptadecyl, and 1-octadecyl diesters of (6-deoxy-alpha-D-gluco-heptopyranosyluronic acid) 6-deoxy-alpha-D-gluco-heptopyranosiduronic acid, a new homolog of trehalosuronic acid, were prepared by two procedures. One procedure involved conversion of the peracetylated acid into its dichloride, reaction of the latter with the alkanols, and acid-catalyzed deacetylation of the products, whereas the other consisted of reaction of alkyl mesylates with the potassium salt of the unprotected acid.
- Baer,Breton
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- Enantiomeric synthesis of natural alkylglycerols and their antibacterial and antibiofilm activities
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Alkylglycerols (AKGs) are bioactive natural compounds that vary by alkyl chain length and degree of unsaturation, and their absolute configuration is 2S. Three AKGs (5l–5n) were synthesised in enantiomerically pure form, and were characterised for the first time together with 12 other known and naturally occurring AKGs (5a–5k, 5o). Their structures were established using 1H and 13C APT NMR with 2D-NMR, ESI-MS or HRESI-MS and optical rotation data, and they were tested for their antibacterial and antibiofilm activities. AKGs 5a–5m and 5o showed activity against five clinical isolates and P. aeruginosa ATCC 15442, with MIC values in the range of 15–125 μg/mL. In addition, at half of the MIC, most of the AKGs reduced S. aureus biofilm formation in the range of 23%–99% and P. aeruginosa ATCC 15442 biofilm formation in the range of 14%–64%. The antibiofilm activity of the AKGs assessed in this work had not previously been studied.
- Fernández Montoya, Deicy J.,Contreras Jordan, Luis A.,Moreno-Murillo, Bárbara,Silva-Gómez, Edelberto,Mayorga-Wandurraga, Humberto
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p. 2544 - 2550
(2019/11/13)
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- NEW ANTIVIRAL ACYCLONUCLEOSIDE ANALOGUES
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The present invention concerns a compound having the following formula (I): as well as its use as a medicament, especially for its use for treating viral infections.
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Page/Page column 32-33
(2019/11/12)
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- Total Synthesis of Myrmekioside A, a Mono-O-alkyl-diglycosylglycerol from Marine Sponge Myrmekioderma sp.
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Myrmekioside A, which was isolated from the marine sponge Myrmekioderma sp. as a member of the family of natural mono-O-alkyl-diglycosylglycerols, and which has a strong reversion effect on the tumor cell morphology of ras-transformed cells at 5 μg/mL, wa
- Zhang, Jun,Li, Chunxia,Sun, Linlin,Yu, Guangli,Guan, Huashi
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p. 4246 - 4253
(2015/06/30)
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- Lipid Compounds Targeting VLA-4
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The invention relates to the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein n, G, W, X, Y, and R1 are defined in the detailed description and claims. The compounds of formula I bind to or associate with VLA-4 and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing VLA-4.
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Paragraph 0172-0173
(2013/04/10)
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- A carborane-derivative "click" reaction under heterogeneous conditions for the synthesis of a promising lipophilic MRI/GdBNCT agent
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In this study, the Huisgen reaction has been used to functionalise a carborane cage with a lipophilic moiety and a 1,4,7,10-tetraazacyclododecane-1, 4,7,10-tetraacetic acid (DOTA) ligand to obtain a new Gd boron neutron-capture therapy (BNCT)/magnetic res
- Toppino, Antonio,Bova, Maria Elena,Crich, Simonetta Geninatti,Alberti, Diego,Diana, Eliano,Barge, Alessandro,Aime, Silvio,Venturello, Paolo,Deagostino, Annamaria
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supporting information
p. 721 - 728
(2013/02/23)
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- Phosphonate Ester Derivatives and Methods of Synthesis Thereof
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The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods accor
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Page/Page column 17
(2012/03/26)
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- Synthesis and antileishmanial activity of lipidic amino alcohols
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In this work, a number of lipidic amino alcohols wereas synthesized and evaluated in vitro on cultures of Leishmania amazonensis and Leishmania chagasi. Nine amino alcohols showed inhibition of L. chagasi growth, and seven of them showed inhibition of L. amazonensis with IC50 below 10 μm. Compound 11f was more active than the reference drug amphotericin B against L. chagasi promastigote forms.
- Coimbra, Elaine S.,De Almeida, Mauro V.,Junior, Celso O. R.,Taveira, Aline F.,Da Costa, Cristiane F.,De Almeida, Ana C.,Reis, Elaine F. C.,Da Silva, Adilson D.
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scheme or table
p. 233 - 235
(2010/12/20)
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- Preparation and antitubercular activities of alkylated amino alcohols and their glycosylated derivatives
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A series of N- and C-alkylated amino alcohols and of their protected galactopyranosyl derivatives was synthesized and evaluated for antitubercular activity. Five of these compounds displayed good activity, with a MIC below 12.5 μg/mL. The presence of the carbohydrate slightly affected the antibacterial activity.
- Taveira, Aline F.,Hyaric, Mireille Le,Reis, Elaine F.C.,Araujo, Debora P.,Ferreira, Ana Paula,de Souza, Maria Aparecida,Alves, Livia L.,Lourenco, Maria C.S.,Vicente, Felipe Rodrigues C.,de Almeida, Mauro V.
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p. 7789 - 7794
(2008/04/05)
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- Hypocholesterolemic activity of hesperetin derivatives
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Hesperetin ester and ether derivatives possessing a long alkyl chain were synthesized for examining their hypocholesterolemic activities in high cholesterol-fed mice. Hesperetin 7-O-lauryl ether (4b) and hesperetin 7-O-oleyl ether (4e) exhibited strong cholesterol-lowering effects.
- Jeong, Tae-Sook,Kim, Eun Eai,Lee, Chul-Ho,Oh, Jung-Hoon,Moon, Surk-Sik,Lee, Woo Song,Oh, Goo-Taeg,Lee, Sangku,Bok, Song-Hae
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p. 2663 - 2665
(2007/10/03)
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- Compositions and methods using novel substituted imidazolium lipids
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Compounds of the formula: are provided, in which R1 and R2 each independently represent a C8-C24 saturated or unsaturated hydrocarbon chain, which is optionally interrupted by from 1 to 3 heteroatom moieties, such as -O-, -S-, -NH- and -NR-. The symbol X represents -CH2-, -O-, -S-, -NH- or -NR-. The R group for each of the -NR- moieties represents an alkyl group having from 1 to 4 carbon atoms. Finally, the subscript n represents the integer 1 or 2, and A- represents an anion, preferably chloride or citrate.
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- Scavenger assisted combinatorial process for preparing libraries of tertiary amine compounds
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This invention relates to a novel solution phase process for the preparation of tertiary amine combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
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- N-substituted glycerophosphoethanolamines
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The present invention relates to novel, therapeutically active fatty alkyl and alkenyl ether glycerophospholipids bearing a 3-(2-imidazolinyl)-2-imidazolinyl or 2-imidazolinyl substituent on the ethanolamine nitrogen, methods of using the compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing same. The novel, therapeutically active compounds and salts of the invention possess anti-tumor, anti-psoriatic, anti-inflammatory, and anti-asthma activities.
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- Stereoselective Synthesis of Long-chain 1-O-(β-D-Maltosyl)-3-O-alkyl-sn-glycerols (Alkyl Glyceryl Ether Lysoglycolipids)
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The synthesis of long-chain 2-O-benzyl-3-O-alkyl-sn-glycerols 5 was improved, making these compounds easily accessible for glycosylation experiments.Glycosylation with α-acetobromomaltose following a modified Koenings-Knorr procedure after removal of the protective groups yielded the title compound 9 in good yields.These compounds represent examples of alkyl glyceryl ether lysoglycolipids.Some properties of these amphiphilic compounds with a nonionic carbohydrate head-group differ not much (critical micell concentration, hemolytic activity), other properties differ very much (antitumor efficiency) from the properties of the analogous compounds with a zwitterionic phosphorylcholine head-group.
- Prinz, Harald,Six, Lambert,Ruess, Klaus-Peter,Lieflaender, Manfred
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p. 217 - 225
(2007/10/02)
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- Conversion of Nitro Paraffins into Aldehydes and Ketones
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The use of potassium permanganate provides a simple and effective means for converting nitro paraffin salts to pure aldehydes and ketones in 81-96 percent yields.Even the carbon-carbon double bond is less readily attacked by permanganate than a nitro paraffin anion.Thus, the salt of ω-nitroundecylene is converted to undecylenic aldehyde in 59 percent yield.
- Kornblum, Nathan,Erickson, Allen S.,Kelly, William J.,Henggeler, Barbara
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p. 4534 - 4538
(2007/10/02)
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