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Sato Chizuru - - 2009
In plants, the mobile signal needed for wound-induced systemic acquired resistance (WSR) has been elusive. The signal compound involved in WSR is supposed to be JA or its derivatives. On the basis of kinetic study of the accumulation of JA or its derivatives, it was discovered that JA, JA-Ile, tuberonic ...
Boga Carla - - 2009
In order to improve the efficacy of doxorubicin (DOXO) in the treatment of hepatocellular carcinomas, the drug was conjugated with lactosaminated human albumin (L-HSA), a hepatotropic drug carrier. Conjugation was performed using the (6-maleimidocaproyl)hydrazone derivative of the drug (DOXO-EMCH). The maleimide group of DOXO-EMCH reacts with the aminoacidic residues of ...
Dangi Bindi - - 2010
17S-HDPAn-6 (17S-hydroxydocosa-4Z,7Z,10Z,13Z,15E-pentaenoic acid) and 10S,17S-HDPAn-6 (10S,17S-dihydroxydocosa-4Z,7Z,11E,13Z,15E-pentaenoic acid) are potent anti-inflammatory resolvins derived from DPAn-6 (docosapentaenoic acid n-6) and are analogous in structure and action to DHA (docosahexaenoic acid)-derived resolvins. These resolvins have proven to be potential drug candidates, albeit with therapeutic profiles that need optimization. The main objectives of this ...
Hiraiwa Yukiko - - 2009
4-Butyl-3-methylphthalic acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted phthalic acids afforded 3-phenylphthalic acid derivatives as potent IMP-1 inhibitors. On the other hand, 3-substituted with 4-hydroxyphenyl phthalic acid derivative displayed a potent combination effect with biapenem (BIPM) against Pseudomonas aeruginosa that produce IMP-1.
Bard Susan - - 2009
Molluscum contagiosum (MC) virus is a common cutaneous infection in the pediatric population, most commonly affecting school-aged children. Spontaneous clearing of lesions usually occurs over time; however, treatment is often sought due to cosmetic significance, pruritus, or concerns of transmission and autoinoculation. Chemical destruction with cantharidin, which is derived from ...
Arrachart Guilhem - - 2009
Two monotrialkoxysilylated compounds that consist of complementary fragments of melamine (M) and cyanuric acid (CA) have been synthesised. The molecular recognition properties of the M and CA fragments through complementary hydrogen bonds (DAD and ADA; D=donor, A=acceptor) are the key factor used to direct the formation of hybrid silica materials ...
Gaywood Alexander P - - 2009
Flash vacuum pyrolysis (FVP) of 2-acetyl-3-azidothiophene gives 3-methylthieno[3,2-c]isoxazole as the major product at a furnace temperature of 350 degrees C whereas at temperatures above 550 degrees C the new heteroindoxyl 4,5-dihydrothieno[3,2-b]pyrrol-6-one is exclusively formed. The heteroindoxyl exists predominantly as the keto tautomer. It is O-protonated by TFA, N-acetylated by acetic ...
Van Cleemput Marjan - - 2009
Hop acids, a family of bitter compounds derived from the hop plant (Humulus lupulus), have been reported to exert a wide range of effects, both in vitro and in vivo. They exhibit potential anticancer activity by inhibiting cell proliferation and angiogenesis, by inducing apoptosis, and by increasing the expression of ...
Chauhan H P S - - 2009
Replacement reactions of toluene-3,4-dithiolatoantimony(III) chloride with oxygen and/or sulphur donor ligands like benzoic acid, thiobenzoic acid, thioacetic acid, phenol, thiophenol, sodium salicylate and thio glycolic acid in 1:1 molar ratio as well as disodium oxalate in 2:1 molar ratio in refluxing anhydrous benzene yielded toluene-3,4-dithiolatoantimony(III) mono oxo and/or thio carboxylic ...
Heiser C - - 2010
In this case report a patient with anosmia due to occupational exposure to barbituric acid will be presented. Occupational exposure to high concentrations of barbituric acid resulted in bloody nasal secretion and nasal itching with immediate onset following exposure. After several days of exposure, a progressive loss of smell resulted ...
Wang Wei - - 2009
Several amino acid derived iminodicarboxylicacid monomethylesters have been converted into a small array of amide derivatives. Sequentially, we were using an Ugi reaction of alpha-amino acids, followed by a mild and efficient amidation. Thus we added to this well-known Ugi scaffold another dimension of diversity, thereby enhancing it is potentially ...
Lipson Victoria V - - 2009
A general review (138 references) focused on the recent advances in the application of Meldrum's acid reactivity for synthesis of diverse pyridine and pyrimidine derivatives, mostly small and drug-like molecules is presented.
de Sá Matheus Santos - - 2009
Malaria is one of the most important tropical diseases and mainly affects populations living in developing countries. Reduced sensitivity of Plasmodium sp. to formerly recommended antimalarial drugs places an increasing burden on malaria control programs as well as on national health systems in endemic countries. The present study aims to ...
Hojabri Leila - - 2009
A new linear saturated terminal diisocyanate was synthesized from oleic acid via Curtius rearrangement, and its chemical structure was identified by FTIR, (1)H and (13)C NMR, and MS. The feasibility of utilizing this new diisocyanate for the production of polyurethanes (PUs) was demonstrated by reacting it with commercial petroleum-derived polyols ...
Ekkati A R - - 2010
N-Acetyl-AA(amino acid)-NHtBu derivatives of all 20 naturally occurring amino acids have been synthesized. Syntheses were performed via solution-phase methodology with yields that allow for access to gram quantities of substrates, in most cases. Syntheses include the coupling of a hindered amine, tert-butylamine, with each amino acid, either directly or in ...
Gavernet Luciana - - 2009
Sulfamides are promising functions for the design of new antiepileptic drugs ( Bioorg. Med. Chem. 2007, 15, 1556-1567; 5604-5614 ). Following previous research in this line, a set of amino acid-derived sulfamides has been designed, synthesized, and tested as new anticonvulsant compounds. The experimental data confirmed the ability of some ...
Liu Boyang - - 2009
1-Beta-D-arabinofuranosylcytosine (Ara-C, Cytarabine) is one of the drugs used for acute nonlymphocytic leukemia (ANLL). However, the bioavailability of Ara-C is relatively low due to its low lipophilicity. In order to improve the lipophilicity and bioavailability of Ara-C, a series of N(4) derivatives of Ara-C, i.e., (fatty acid)-(amino acid)-Ara-C analogues, were ...
Watanabe Takumi - - 2009
Boronic acid derivatives of tyropeptin were synthesized with TP-110 as the lead compound. Due to the lability of the aminoboronic acid moiety, careful design of the deprotection and coupling sequence was required. Liquid-liquid partition chromatography was found to be a powerful tool for purification of compounds of this class. The ...
Bereczki Laura - - 2009
Optical resolution methods were established for racemic 1-(1-naphthyl) ethylamine. The resolving agents were synthesized by N-derivatizing (R)-1-(1-naphthyl) ethylamine with dicarboxylic acids. Oxalic, malonic, and succinic acid derivatives were found to be suitable resolving agents. These resolutions are parallel to a series of optical resolutions of 1-phenylethylamine which had been previously ...
Neumann Kerstin - - 2009
Tetramic acid derivatives are an important class of nitrogen heterocycles with a pyrrolidine-2,4-dione core as a key structural motif. From the sponge-derived fungus Beauveria bassiana, a new equisetin-like tetramic acid derivative, beauversetin (1), was isolated. The sea weed-derived fungus Microdiplodia sp. produced the tetramic acid derivative 2 (Sch210972) which was ...
Schranz M E - - 2009
In the Brassicaceae, glucosinolates influence the feeding, reproduction and development of many insect herbivores. Glucosinolate production and effects on herbivore feeding have been extensively studied in the model species, Arabidopsis thaliana and Brassica crops, both of which constitutively produce leaf glucosinolates mostly derived from the amino acid, methionine. Much less ...
Gasser Gilles - - 2009
The rational, sequential synthesis of two hetero-bimetallic derivatives of the amino acid phenylalanine and one thymine (T) peptide nucleic acid (PNA) monomer is reported. Ferrocene carboxylic acid and (eta-ethene)bis(triphenylphosphine)platinum(0) were successfully reacted with propargylamide amino acid (1a and 1b) or a T PNA monomer derivative (6) to give the expected ...
Béthencourt Mathilde I - - 2009
Self-assembled monolayers (SAMs) on gold derived from the direct adsorption of thioacetic acid S-decyl ester (C10SAc) and thioacetic acid S-octadecyl ester (C18SAc) were compared to the corresponding SAMs derived from the analogous adsorption n-decanethiol (C10SH) and n-octadecanethiol (C18SH). All SAMs were characterized using ellipsometry, contact angle goniometry, polarization modulation infrared ...
Sille Július - - 2009
The B3LYP/6-311+G(d,p) method and three ONIOM extrapolation methods ONIOM (B3LYP/6-311+G(d,p): AM1); ONIOM(B3LYP/6-311+G(d,p): MNDO); ONIOM (B3LYP/6-311+G(d,p): HF/3-21G(d)) were used to characterize the complexes of Zn2+ cation with anionic sulfonylated amino acid hydroxamates (RSO2NH-AA-CON(-)OH), possessing an unsubstituted RSO2NH-amino acyl moiety. According to the R moiety we distinguish between pentafluorophenyl and 4-methoxyphenyl derivates. ...
Barkei John J - - 2009
Viomycin and capreomycin are members of the tuberactinomycin family of antituberculosis drugs. As with many antibacterial drugs, resistance to the tuberactinomycins is problematic in treating tuberculosis; this makes the development of new derivatives of these antibiotics to combat this resistance of utmost importance. To take steps towards developing new derivatives ...
Accetta Alessandro - - 2009
The synthesis of C5 linked uracil dimers was carried out according to a model developed in order to bind adenine in DNA. N1-Alkylated uracil derivatives were synthesized from isoorotic acid (uracil-5-carboxylic acid) or thymine. The carboxylic acid derivatives were condensed with diamines in order to produce dimeric compounds or with ...
Thompson Christina M - - 2009
Small molecule inhibitors of apoptosis hold considerable promise for the treatment of a host of diseases, including neurodegeneration, myocardial infarction, and stroke. Many compounds that delay or prevent apoptotic death either reduce the amount of cellular reactive oxygen species (ROS) or are direct inhibitors of caspases. With the goal of ...
Fülöp Ferenc - - 2009
The syntheses and transformations of 4-hydroxyquinoline-2-carboxylic acid, kynurenic acid, are reviewed, and special attention is paid to the pharmacological activities and pharmaceutical applications of its derivatives.
Tsimihodimos V - - 2009
Fenofibrate represents the most commonly used fibric acid derivative. The drug exerts its metabolic effects by modulating the expression of several genes involved in lipoprotein metabolism. In addition, numerous studies suggest that fenofibrate may also affect the progression of the atherosclerotic process by several lipid-independent mechanisms. This review considers the ...
Ma Chao-Mei - - 2009
PURPOSE: To evaluate oleanolic acid derivatives on liver disease related bioactivities, 29 oleanolic acid derivatives of several series were tested for their inhibitory activity on hepatitis C viral protease and for their cytotoxic effects on Hep G2 cells. RESULTS: The amino derivatives showed potent cytotoxicity, among which, the beta-amino isomer ...
Schalock Peter C - - 2009
Lichen-derived additives to commercial products are becoming a more frequent cause of allergic contact dermatitis. The most common lichen-derived additives are usnic acid and oak moss absolute. Both are useful for screening patients using "natural" or "botanical" products that may contain lichen-derived additives.
Li Jun-Feng - - 2009
Oleanolic acid with anti-bone resorption effect was an active component discovered in a medicinal plant of Achyranthes bidentata. A series of heterocyclic derivatives of oleanolic acid including indole, pyrazine, quinoxaline, quinoline moieties and their natural amino acid amides were synthesized. Their inhibitory activity on the formation of osteoclast-like multinucleated cells ...
Maas Mareike - - 2009
From the ethyl acetate soluble fraction of a methanol/water extract of the herb Eupatorium perfoliatum L. (Asteraceae) six caffeic acid derivatives have been isolated and identified by 1D- and 2D-NMR spectroscopic data. Besides the common quinic acid derivatives 5-caffeoylquinic acid (chlorogenic acid), 3-caffeoylquinic acid (neochlorogenic acid) and 3,5-dicaffeoylquinic acid, three ...
Shen Wei - - 2009
5'-O-D- and L-amino acid derivatives and 5'-O-(D- and L-amino acid methyl ester phosphoramidate) derivatives of vidarabine (ara-A) were synthesized as vidarabine prodrugs. Some compounds were equi- or more potent in vitro than vidarabine against two pox viruses and their uptake by cultured cells was improved compared to the parent drug.
Kaplancikli Zafer Asim - - 2008
New hydrazide derivatives of imidazo[1,2-a]pyridine have been synthesized and evaluated for anticandidal activity. The reaction of imidazo[1,2-a]pyridine-2-carboxylic acid hydrazides with various benzaldehydes gave N-(benzylidene)imidazo[ 1,2-a]pyridine-2-carboxylic acid hydrazide derivatives. Their anticandidal activities against Candida albicans and Candida glabrata (isolates obtained from Osmangazi University, Faculty of Medicine, Eskisehir, Turkey), Candida albicans (ATCC ...
Chomcheon Porntep - - 2009
The endophytic mitosporic Dothideomycete sp. LRUB20 was found to produce pyrone derivatives, dothideopyrones A-D (1, 3, 4, and 5), together with seven known compounds, including questin (9), asterric acid (10), methyl asterrate (11), sulochrin (12), and eugenitin (13), 6-hydroxymethyleugenitin (14), and cis, trans-muconic acid (15). Dothideopyrone D (5) and its ...
Nishshanka Upul - - 2008
Diesters of ortho-hydroxybenzoic acid (salicylic acid) made with glutaric, adipic, and pimelic acids are the monomers of some potential drug candidates for aspirin patches. Collision-induced dissociation (CID) spectra of negative ion derived from these compounds show a 120-Da 'neutral loss' specific to the ortho isomers. In contrast, the anions derived ...
Brozic P - - 2009
Human hydroxysteroid dehydrogenase (HSD) AKR1C1 is a member of the aldo-keto reductase superfamily, and it functions mainly as a 20alpha-HSD. It catalyzes the reduction of the potent progesterone to the weak 20alpha-hydroxyprogesterone, and of 3alpha,5alpha-tetrahydroprogesterone (5alpha-THP; allopregnanolone) to 5alpha-pregnane-3alpha,20alpha-diol. AKR1C1 thus decreases the levels of progesterone and 5alpha-THP in peripheral ...
Malamidou-Xenikaki Elizabeth - - 2008
Although 1,3-dioxoindane-2-carboxylic acid is highly unstable, its enamino derivatives can be isolated by careful hydrolysis of their esters with 2,4-dihydroxy-1,4-naphthoquinone. Crystal structure determination reveals the formation of two intramolecular hydrogen bonds, offering thus a possible explanation for the stability of these acids.
Onoue Satomi - - 2008
Drug-induced phototoxic skin responses have been recognized as undesirable side effects, and as we previously proposed the determination of reactive oxygen species (ROS) from photo-irradiated compounds can be effective for the prediction of phototoxic potential. In this investigation, we evaluated the photosensitizing properties of imidazopyridine derivative, a novel 5-HT(4) partial ...
Sha J - - 2008
Avian blastodermal cells at stage X are used to produce interspecies chimeras for heterogenous poultry reproduction. However, recipient-derived inner perivitelline layer (IPVL)-enclosed donor-derived ova may affect the efficiency of germline transmission via chimera. Among the proteins in the IPVL, zona pellucida protein C (ZPC) plays an important role in sperm-egg ...
Miura Tomoaki - - 2008
The design and synthesis of novel 14- to 16-membered 11-azalides starting from 16-membered macrolides are reported. A linear 9-formylcarboxylic acid was isolated via a mobile dialdehyde previously reported. Sequential macrocyclization of the formylcarboxylic acid with amino alcohol followed by deprotection afforded corresponding 14- to 16-membered azalides. On the other hand, ...
Bavikar Sudhir N - - 2008
Tetrapeptides derived from glycine and beta-alanine were hooked at the C-3beta position of the modified cholic acid to realize novel linear tetrapeptide-linked cholic acid derivatives. All the synthesized compounds were tested against a wide variety of microorganisms (gram-negative bacteria, gram-positive bacteria and fungi) and their cytotoxicity was evaluated against human ...
Motiur Rahman A F M - - 2008
The 2,2-dimethyl-2H-pyran-derived alkaloids acronycine and its demethylated congeners were prepared in three steps from anthranilic acid and phloroglucinol. The phenylboronic acid-mediated interamolecular cyclization reaction of 1,3-dihydroxyacridone and 3-methylbut-2-enal was employed as a key step, which was also applied to the synthesis of related cytotoxic benzo[b]acronycine. Inhibitory activities of the compounds ...
Sassaki Guilherme L - - 2008
The structure of glycoconjugates has been determined by several chromatographic methods, however gas chromatography-mass spectrometry (GC-MS) has been widely used to identify and quantify the volatile trimethylsilyl and fluoroacyl derivatives. Adapting the reduction/acetylation strategies, we had performed the derivatization of all monosaccharide class, as well as amino acids and OH-fatty ...
Duan Wengui - - 2009
A new type of chitosan derivative, dehydroabietic acid-modified chitosan (DAMC), was synthesized by the acylation reaction of chitosan with dehydroabietic acid chloride (DHAC) under microwave irradiation. The resulting product (DAMC) was characterized by FT-IR, UV, (1)H NMR, X-ray diffraction (XRD), scanning electron microscopy (SEM), thermal gravimetric analysis (TGA), and elemental ...
Smith Aoife - - 2008
A series of fatty acid ester and ether derivatives have been chemically synthesised based on carbohydrate and non-carbohydrate polyhydroxylated scaffolds. The synthesised compounds, along with their corresponding fatty acid monoglyceride antimicrobials, were evaluated for antimicrobial activity against Staphylococcus aureus and Escherichia coli. Of the derivatives synthesised, several of the carbohydrate-based ...
Le Corre Laurent - - 2008
Various substituents could be diastereoselectively introduced into the 5-position of pipecolic acid via electrophilic or free-radical-initiated addition to the carbon-carbon double bond of endocyclic enecarbamates derived from pipecolic acid. This study allowed the diastereoselective synthesis of both cis- and trans-5-guanidino pipecolates, which were designed as constrained arginine mimetics and whose ...
Giroux Simon - - 2008
Synthesis and testing of dafachronic acid A ( 1) and its derivatives 2 and 3 have revealed that 1, and not a further oxidation product, is the natural ligand for the DAF-12 receptor of Caenorhabditis elegans.
Kumar Indresh - - 2008
Single-walled carbon nanotubes (SWCNTs) were chemically functionalized with amino acid-based moieties. The covalent functionalization of alkyne-derived SWCNTs with well defined azides derived from amino acids was accomplished through Cu(I)-catalyzed Huisgen [3+2] dipolar cycloaddition click chemistry. Transmission electron microscopy, Raman spectroscopy, and infrared spectroscopic measurements confirmed the functionalization of SWCNTs by ...
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