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Mendes Gabriella - - 2011
In this paper, we evaluated the antiviral activity against HMPV replication of crude extract of the marine algae Stypopodium zonale and of two meroditerpenoids obtained from it, atomaric acid and epitaondiol, and a methyl ester derivative of atomaric acid. Their selectivity indexes were 20.78, >56.81, 49.26 and 12.82, respectively. Compared ...
Wójciak-Kosior Magdalena - - 2011
In this article, we look at how ursolic and oleanolic acids can be used for the purpose of quality control of natural products used in dermatocosmetology as well as of various other therapeutic preparations. Ursolic acid (UA) and oleanolic acid (OA) are pentacyclic triterpenes and they are constituents of many ...
Basanagouda M - - 2011
Coumarin-4-acetic acids have been synthesized from various phenols and citric acid under Pechmann cyclisation conditions. All the compounds have been evaluated for antiinflammatory and analgesic activity in acute models. Compounds have also been evaluated for their ulcerogenic potential. Using the computer program, prediction of activity spectra for substances, prediction results ...
Das Undurti N - - 2011
Previous studies showed that γ-linolenic acid (GLA, 18: 3 ω-6), arachidonic acid (AA, 20:4 ω-6), eicosapentaenoic acid (EPA, 20: 5 ω-3) and docosahexaenoic acid (DHA, 22:6 ω-3) have selective tumoricidal action. In the present study, it was observed that dihomo-gamma-linolenic acid (DGLA) and AA, EPA and DHA have cytotoxic action ...
Aiello Anna - - 2011
Chemical analysis of the Mediterranean ascidian Polyandrocarpa zorritensis (Van Name 1931) resulted in the isolation of a series of molecules including two monoindole alkaloids, 3-indolylglyoxylic acid (3) and its methyl ester (4), 4-hydroxy-3-methoxyphenylglyoxylic acid methyl ester (1) and a new alkaloid we named zorrimidazolone (2). The structure of the novel ...
Ion Gabriela - - 2011
The Western diet is high in omega-6 fatty acids and low in omega-3 fatty acids. Canola oil contains a healthier omega 3 to omega 6 ratio than corn oil. Jurkat T leukemia cells were treated with free fatty acids mixtures in ratios mimicking that found in commercially available canola oil ...
Zofou Denis - - 2011
Malaria is a major public health threat in Africa, and traditional medicine continues to play a key role in its control especially in rural areas. A bioassay-guided fractionation was carried out in order to evaluate the anti-malarial potential and the safety of the methanol extract of the Hypericum lanceolatum stem ...
Rae James - - 2011
Mammalian cells store excess fatty acids as neutral lipids in specialised organelles called lipid droplets (LDs). Using a simple cell-based assay and open-source software we established a high throughput screen for LD formation in A431 cells in order to identify small bioactive molecules affecting lipid storage. Screening an n-butanol extract ...
Delgado-Pando G - - 2010
Healthier lipid pâtés were formulated by reducing the fat content and/or replacing the pork backfat by a healthier oil combination (olive, linseed and fish oils) and konjac gel (0-15%). The reformulation results were evaluated by composition (proximate analysis and fatty acid profile), technological properties (emulsion stability, colour, and texture), microbiological ...
Mascari T M - - 2010
The purpose of this study was to evaluate the use of boric acid, imidacloprid, ivermectin, or abamectin incorporated into sugar baits as oral toxicants for adult phlebotomine sand flies. Variable toxicity of insecticide-sugar bait solutions to adult male and female sand flies was demonstrated, based on male female median lethal ...
Hondrodimou O - - 2011
The effect of natamycin as a fungal control agent in natural black olive fermentation according to the traditional anaerobic system was studied. Black Conservolea olives were subjected to spontaneous fermentation in 8% (w/v) NaCl brine solution (control treatment) or brine supplemented with 0.01% (w/v) natamycin (active compound) for an overall ...
Yang Shiqiong - - 2011
A series of sulf(on)ate and phosph(on)ate amino acid phosphoramidate analogues of deoxynucleotides were synthesized as potential substrates for HIV-1 reverse transcriptase. Taurine, l-cysteic acid, 3-phosphono-l-alanine, O-sulfonato-l-serine, and O-phospho-l-serine were investigated as leaving groups in an enzyme catalyzed DNA synthesis protocol. Among these analogues, the phosphonate congener performed best and 3-phosphono-l-alanine ...
Owusu-Ansah Ernest - - 2011
(S)-4,4-Dichloro-3-methylbutanoic acid was prepared in 51% overall yield from commercially available starting materials using an organocatalytic transfer hydrogenation to 4,4-dichloro-3-methylbut-2-enal in the key step. The (S)-dichloro acid was used as an intermediate in the first total synthesis of dysideaproline E and a diastereomer confirming the structure of the natural product.
Jeong Yunkyung - - 2011
The SO(3)H-tethered imidazolium and triazolium salts, nonvolatile and recyclable Brønsted acidic ionic liquids, efficiently mediate intramolecular hydroalkoxylations of alkenyl alcohols. They have been successfully employed in the synthesis of (±)-centrolobine.
van Delft Pieter - - 2010
The conjugation of a ribonucleic acid 16-mer with the cationic amphiphilic peptide penetratin and an anionic hyaluronan tetrasaccharide by means of Cu-free "click" chemistry is reported. The alkyne-functionalized 16-mer was prepared by automated solid-phase synthesis, using a newly developed strained cyclooctyne phosphoramidite in the final coupling. Cycloaddition of the alkyne ...
Vervisch Karel K Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, - - 2010
2-(2-Cyano-2-phenylethyl)aziridines were converted into novel cis- and trans-2-chloromethyl-4-phenylpiperidine-4-carbonitriles via alkylation with 1-bromo-2-chloroethane followed by microwave-assisted 6-exo-tet cyclization and regiospecific ring opening. The latter piperidines were used as eligible substrates for the synthesis of stereodefined 2-chloromethyl-, 2-hydroxymethyl-, and 2-carboxymethyl-4-phenylpiperidine-4-carboxylic acids, 2-hydroxymethyl-4-phenylpiperidine-4-carbonitriles, 3-hydroxy-5-phenylazepane-5-carbonitriles, and 5-phenyl-2,7-diazabicyclo[3.3.1]nonanes.
Xu Zhengren Z State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, - - 2010
The stereocontrolled total synthesis of clavicipitic acid and aurantioclavine from a common azepino[5,4,3-cd]-indole intermediate is reported. This key azepinoindole nucleus was constructed via a one-pot Heck/Boc-deprotection/aminocyclization process from the 4-iodotryptophan derivative, which was assembled by a Pd-catalyzed indole synthesis procedure. After two or three additional deprotection steps from the azepinoindole ...
Bouillère Francelin - - 2011
The synthesis of orthogonally protected diastereo- and enantiopure β,γ-diamino acids starting from natural α-amino acids is described, as well as its application to the synthesis of fully protected 3-deoxyaminostatine.
Abbas Hafiz G - - 2011
Sodium 2-{6-(4-chlorophenoxy)hexyl}oxirane-2-carboxylate (Etomoxir) inhibits transport of fatty acids via the carnitine shuttle into mitochondria of muscle cells and prevents long chain fatty acids from providing energy through β-oxidation especially for muscle contraction. The objective of this synthesis is to develop a method for radioiodination of Etomoxir in order to explore ...
Fang Chao - - 2010
Both C19 and C34 spiroketal domains of okadaic acid were assembled using gold(I) chloride catalyzed spiroketalizations, and the two resulting fragments were coupled to give the C15-C38 fragment of okadaic acid, a known intermediate for the total synthesis of this important natural product.
Colbert Christopher L - - 2010
Spot 14 (S14) is a protein that is abundantly expressed in lipogenic tissues and is regulated in a manner similar to other enzymes involved in fatty acid synthesis. Deletion of S14 in mice decreased lipid synthesis in lactating mammary tissue, but the mechanism of S14's action is unknown. Here we ...
McFadden J W - - 2010
Liver X receptor (LXR) is a nuclear receptor and a known regulator of lipid synthesis in rodents; however, the role of LXR in the regulation of fatty acid synthesis in bovine mammary epithelial cells has not yet been defined. The objective of the study was to evaluate the effect of ...
Scott Erin M - - 2010
The enzyme homocitrate synthase (HCS) catalyzes the first step in lysine biosynthesis, and early biochemical data placed it in the cytoplasm or mitochondria, where most amino acid synthesis occurs. It was therefore surprising when refined fractionation techniques and specific immunoreagents clearly demonstrated its localization to the nucleus. These observations raised ...
Yao Nianhuan - - 2010
The synthesis of glycosylated Fmoc amino acids by reaction of mono- and disaccharide peracetates with Fmoc amino acids having free carboxyl groups was rapidly promoted by Lewis acids (SnCl(4), BF(3)·Et(2)O) under microwave irradiation. The products are useful building blocks for the synthesis of glycopeptides.
Yang Xueying - - 2010
Herbicides that affect lipid metabolism have been used commercially for many years. Here, napropamide, diphenamid, dimethachlor and cafenstrole are compared; these have all been classified by the Herbicide Resistance Action Committee (HRAC) as K(3) herbicides and inhibitors of cell division and/or synthesis of very-long-chain fatty acids (VLCFAs). In addition, spiro-decanedione ...
Wu Boshen - - 2010
Two new routes to the C(1-10) carboxylic acid core of taurospongin A are presented. In the first route, overall asymmetric hydration of a C(2)-C(3) alkene is achieved by Sharpless AD and selective deoxygenation at C(2); in the second route, the C(3) stereogenic center is set by Tietze asymmetric allylation. A ...
Cheruku Pradeep - - 2010
Synthesis of the marine natural products motualevic acids A, E, and analogs in which modifications have been made to the omega-brominated lipid (E)-14,14-dibromotetra-deca-2,13-dienoic acid or amino acid unit are reported, together with antimicrobial activities against Staphylococcus aureus, methicillin-resistant S. aureus, Enterococcus faecium, and vancomycin-resistant Enterococcus.
Ohkubo Akihiro - - 2010
Amidine-type protecting groups, i.e., N,N-dimethylformamidine (dmf) and N,N-dibutylformamidine (dbf) groups, introduced into nucleobases were rapidly removed under mild acidic conditions using imidazolium triflate (IMT) or 1-hydroxybenztriazole (HOBt). This new deprotection strategy allowed a 2'-O-methyl-RNA derivative bearing a base-labile group to be efficiently synthesized using a silyl-type linker. It was also ...
Bew Sean P - - 2010
Recent years have seen a huge surge of interest in the application of alkyne-derived motifs for so-called "click" chemistry. Given the critical importance of amino acids in organic synthesis as well as their myriad of applications in "click" chemistry it is interesting to note that the synthesis of C-propargyl derived ...
Hanessian Stephen - - 2010
The asymmetric synthesis of a carbocyclic delta-amino acid representing the P(2)/P(3) subunit of a nonpeptidic truncated peptidomimetic molecule is described relying on two independent approaches.
Alonso Ana Paula - - 2010
The efficiency with which developing maize embryos convert substrates into seed storage reserves was determined to be 57-71%, by incubating developing maize embryos with uniformly labeled 14C substrates and measuring their conversion to CO2 and biomass products. To map the pattern of metabolic fluxes underlying this efficiency, maize embryos were ...
Ecker Josef - - 2010
Monocytes are precursors of macrophages. Here we demonstrate that macrophage colony-stimulating factor (M-CSF)-dependent differentiation of primary human monocytes from healthy volunteers induces transcription of SREBP-1c target genes required for fatty acid (FA) biosynthesis and impairs transcription of SREBP-2 target genes required for cholesterol synthesis. Detailed lipid metabolic profiling showed that ...
Pearce Oliver M T - - 2010
N-Glycolylneuraminic acid (Neu5Gc) is a non-human sialic acid, which may play a significant role in human pathologies, such as cancer and vascular disease. Further studies into the role of Neu5Gc in human disease are hindered by limited sources of this carbohydrate. Using a chemo-enzymatic approach, Neu5Gc was accessed in six ...
Duan Zhang-Qun - - 2010
The influence of solvents with a wide range of log P (from -0.23 to 4.5) on the positional selectivity of the immobilized lipase Novozym 435 during the esterification of oleic acid with glycerol for 1,3-diolein preparation was investigated. Analysis was performed on the basis of a simplified kinetic model of ...
Oakdale James S - - 2010
Two complementary concise total syntheses of lycogarubin C (1) and lycogalic acid (2, aka chromopyrrolic acid) are detailed utilizing a 1,2,4,5-tetrazine --> 1,2-diazine --> pyrrole Diels-Alder strategy and enlisting acetylenic dienophiles.
Chatterjee Anamitra - - 2010
An efficient synthesis of rac-trichostatic acid (1) and its analogues is reported starting from a commercially available aldehyde. Further manipulations of rac-1 led to rac-trichostatin A (TSA). Construction of the desired molecular architecture entails a two-component union, achieved through an in situ hydroboration followed by a Suzuki-Miyaura coupling with 2. ...
Bindschädler Pascal - - 2010
A divergent de novo synthesis of six differentially protected l-iduronic acid thioglycosides from a common advanced precursor is described. The key step of this synthetic sequence is the stereoselective elongation of dithioacetal protected C5-dialdehyde 11 via a highly diastereoselective MgBr(2).OEt(2)-mediated cyanation. Orthogonally protected l-iduronic acid building blocks obtained by this ...
Radchenko Dmytro S - - 2010
Synthesis of 6-amino-2-azaspiro[3.3]heptane-6-carboxylic acid and 2-azaspiro[3.3]heptane-6-carboxylic acid was performed. Both four-membered rings in the spirocyclic scaffold were constructed by subsequent ring closure of corresponding 1,3-bis-electrophiles at 1,1-C- or 1,1-N-bis-nucleophiles. The two novel amino acids were added to the family of the sterically constrained amino acids for the use in chemistry, ...
Yavari Issa - - 2010
An efficient synthesis of 1-aryl-5-aryl(alkyl)-1,2-dihydro-3H-1,2,4-triazole-3-thiones via reaction between ammonium thiocyanate, acid chlorides, and arylhydrazines is described.
Francais Antoine - - 2010
The first convergent total synthesis of isobongkrekic acid is reported involving three different stereospecific palladium cross-couplings for the formation of the diene units. Access to bongkrekic acid by this route is also demonstrated. These syntheses involve the formation of several potentially general building blocks.
Yadav J S - - 2010
A convergent approach to the total synthesis of pteridic acid A, having potent plant growth regulator activity, is described. Key steps include the desymmetrization of bicyclic olefin with Brown's chiral hydroboration, acid-mediated spiroketalization, and zirconium-catalyzed ethylmagnesation protocol to install the ethyl stereocenter at C14.
Nesvadba Peter - - 2010
Addition of the lithium salt of N-hydroxy-2,2,6,6-tetramethylpiperidine 10 to carbon disulfide and subsequent methylation affords the rearranged dithiocarbonic acid S-methyl-S'-(2,2,6,6-tetramethylpiperidin-1-yl)-ester 9 rather than the expected xanthate ester S-methyl-O'-(2,2,6,6-tetramethylpiperidin-1 -yl)-ester 8. n-Butylacrylate could be polymerized with the novel compound 9 even though the polymerization was not controlled.
Kitayama Takashi - - 2010
A concise synthesis of valerena-4,7(11)-diene with potent sedative activity was achieved in three steps involving, reduction of carboxylic acid, bromination of the resulting alcohol, and reduction of the bromide from valerenic acid in a 63% total yield. This synthetic method makes it possible to provide further materials for biological testing ...
Elizondo-Montemayor Leticia - - 2010
Aim: To assess the plasma phospholipid (PL) fatty acid composition in obese Mexican children and evaluate gender differences and predisposition to health risks. Methods: This was a case-control study of 100 obese and 100 normal-weight children aged 6-12 years. BMI, waist circumference, triceps skinfold, and percentage of body fat were ...
Prajapati M S - - 2010
Leucas aspera commonly known as 'Thumbai' is distributed throughout India from the Himalayas down to Ceylon. The plant is used traditionally as an antipyretic and insecticide. Medicinally, it has been proven to possess various pharmacological activities like antifungal, antioxidant, antimicrobial, antinociceptive and cytotoxic activity. Further, studies reveal the presence of ...
Vaswani Rishi G - - 2009
This paper describes ongoing progress toward the synthesis of the novel indole alkaloid actinophyllic acid via a synthetic strategy that allows for the installation of all C-atoms (highlighted in red) requisite for completion of a total synthesis.
Tarun Alice S - - 2009
Fatty acids are essential components of membranes, and are also involved in cell signalling. Plasmodium, the parasite that causes malaria, scavenges fatty acids from its hosts. However, Plasmodium also possesses enzymes for a prokaryotic-like de novo fatty acid synthesis pathway, which resides in the apicoplast. Recent research has demonstrated that ...
Basso Andrea - - 2009
Research progress is often promoted by unexpected results that open the way to new scenarios. In this communication, an unprecedented condensation of arylacetic acids and isocyanides and the unusual base-mediated rearrangement of the resulting products to give two novel classes of polysubstituted pyrrolones and pyrrolidinediones are reported.
Wu Xiaoxing - - 2009
A Kiyooka aldol condensation of an aldehyde with a trimethylsilyl ketene acetal and the oxazaborolidinone prepared from N-Ts-(S)-valine gives two of the four possible aldol adducts, which were oxidized and deprotected to complete the synthesis of (-)-berkelic acid and (-)-22-epi-berkelic acid. This synthesis establishes the absolute stereochemistry and assigns the ...
Wang Yizhong - - 2009
Six photoreactive tetrazole amino acids were efficiently synthesized either by the de novo Kakehi tetrazole synthesis method or by alkylation of a glycine Schiff base with tetrazole-containing alkyl halides, and four of them showed excellent reactivity toward a simple alkene in the photoinduced 1,3-dipolar cycloaddition reaction in acetonitrile/PBS buffer (1:1) ...
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