156914

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Synthesis and in vitro kinetic study of novel mono-pyridinium oximes as reactivators of organophosphorus (OP) inhibited human acetylcholinesterase (hAChE).

Aditya Kapil Valiveti et al.

Chemico-biological interactions, 237, 125-132 (2015-06-14)

A series of mono pyridinium oximes linked with arenylacetamides as side chains were synthesized and their in vitro reactivation potential was evaluated against human acetylcholinesterase (hAChE) inhibited by organophosphorus inhibitors (OP) such as sarin, VX and tabun. The reactivation data

Isolation, chemical characterization, and free radical scavenging activity of phenolics from Triticum aestivum L. aerial parts.

Iwona Kowalska et al.

Journal of agricultural and food chemistry, 62(46), 11200-11208 (2014-10-31)

Fourteen phenolic compounds (flavonoids and phenolic acids) were isolated and 19 were identified in the aerial parts of Triticum aestivum L. The structures of these compounds were established on the basis of the data obtained by electrospray ionization-mass spectrometry (ESI-MS)

pH-sensitive nanoformulated triptolide as a targeted therapeutic strategy for hepatocellular carcinoma.

Daishun Ling et al.

ACS nano, 8(8), 8027-8039 (2014-08-06)

Hepatocellular carcinoma (HCC) has one of the worst prognoses for survival as it is poorly responsive to both conventional chemotherapy and mechanism-directed therapy. This results from a lack of therapeutic concentration in the tumor tissue coupled with the highly toxic

Antibacterial active compounds from Hypericum ascyron L. induce bacterial cell death through apoptosis pathway.

Xiu-Mei Li et al.

European journal of medicinal chemistry, 96, 436-444 (2015-04-29)

Hypericum ascyron L. has been used as a traditional medicine for the treatment of wounds, swelling, headache, nausea and abscesses in China for thousands of years. However, modern pharmacological studies are still necessary to provide a scientific basis to substantiate

Synthesis and analysis of the anticancer activity of platinum(II) complexes incorporating dipyridoquinoxaline variants.

Benjamin J Pages et al.

Dalton transactions (Cambridge, England : 2003), 43(41), 15566-15575 (2014-09-10)

Eight platinum(II) complexes with anticancer potential have been synthesised and characterised. These complexes are of the type [Pt(I(L))(A(L))](2+), where I(L) is either dipyrido[3,2-f:2',3'-h]quinoxaline (dpq) or 2,3-dimethyl-dpq (23Me2dpq) and A(L) is one of the R,R or S,S isomers of either 1,2-diaminocyclohexane

Toward the discovery of dual HCMV-VZV inhibitors: Synthesis, structure activity relationship analysis, and cytotoxicity studies of long chained 2-uracil-3-yl-N-(4-phenoxyphenyl)acetamides.

Denis A Babkov et al.

Bioorganic & medicinal chemistry, 23(21), 7035-7044 (2015-10-08)

The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives--previously reported inhibitors of human cytomegalovirus (HCMV). Introduction of

Preparation and characterisation of hexamidine salts.

Nicola Parisi et al.

International journal of pharmaceutics, 493(1-2), 404-411 (2015-08-04)

Hexamidine diisethionate (HEX D) has been used in the personal care industry and in a number of over-the-counter (OTC) drug products as an antimicrobial agent since the 1950's. Recently, the compound has also been investigated for its beneficial effects on

Antidiabetic effects of flavonoids from Sophora flavescens EtOAc extract in type 2 diabetic KK-ay mice.

Xinzhou Yang et al.

Journal of ethnopharmacology, 171, 161-170 (2015-06-09)

Bitter and cold Chinese medicines have been long used for the treatment for diabetes mellitus (DM) for thousands of years in China. The roots of Sophora flavescens Ait., one of bitter and cold Chinese medicines commonly used to remove lung

Self-Assembly of Catecholic Moiety-Containing Cationic Random Acrylic Copolymers.

Vincenzo Taresco et al.

The journal of physical chemistry. B, 119(26), 8369-8379 (2015-06-16)

Amphiphilic polyelectrolytes (APEs), exhibiting particular self-association properties in aqueous media, can be used in different industrial applications, including drug delivery systems. Their typical core-shell structure (micelle) depends on the balance of interactions between hydrophobic and ionizable monomer units. In this

Correlation of the antimicrobial activity of salicylaldehydes with broadening of the NMR signal of the hydroxyl proton. Possible involvement of proton exchange processes in the antimicrobial activity.

Hannu Elo et al.

European journal of medicinal chemistry, 92, 750-753 (2015-01-27)

Certain substituted salicylaldehydes are potent antibacterial and antifungal agents and some of them merit consideration as potential chemotherapeutic agents against Candida infections, but their mechanism of action has remained obscure. We report here a distinct correlation between broadening of the

Synthesis and Biological Evaluation of N-Aryl-5-aryloxazol-2-amine Derivatives as 5-Lipoxygenase Inhibitors.

Jee Hee Suh et al.

Chemical & pharmaceutical bulletin, 63(8), 573-578 (2015-06-05)

We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazole

Novel heteroaryl phosphonicdiamides PTPs inhibitors as anti-hyperglycemic agents.

Kuruva Chandra Sekhar et al.

Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 22, 76-76 (2014-12-30)

Chronic and oral administration of benzylamine improves glucose tolerance. Picolylamine is a selective functional antagonist of the human adenosine A2B receptor. Phosphonic diamide derivatives enhance the cellular permeability and in turn their biological activities. A series of heteroaryl phosphonicdiamide derivatives

DMSO induces dehydration near lipid membrane surfaces.

Chi-Yuan Cheng et al.

Biophysical journal, 109(2), 330-339 (2015-07-23)

Dimethyl sulfoxide (DMSO) has been broadly used in biology as a cosolvent, a cryoprotectant, and an enhancer of membrane permeability, leading to the general assumption that DMSO-induced structural changes in cell membranes and their hydration water play important functional roles.

Ionic liquid versus prodrug strategy to address formulation challenges.

Anja Balk et al.

Pharmaceutical research, 32(6), 2154-2167 (2014-12-24)

A poorly water soluble acidic active pharmaceutical ingredient (API) was transformed into an ionic liquid (IL) aiming at faster and higher oral availability in comparison to a prodrug. API preparations were characterized in solid state by single crystal and powder

Sulfation modulates the cell uptake, antiradical activity and biological effects of flavonoids in vitro: An examination of quercetin, isoquercitrin and taxifolin.

Lenka Roubalová et al.

Bioorganic & medicinal chemistry, 23(17), 5402-5409 (2015-08-12)

Quercetin 3'-O-sulfate is one of the main metabolites of the natural flavonoid quercetin in humans. This study was designed to prepare quercetin 3'-O-sulfate (1), isoquercitrin 4'-O-sulfate (2) and taxifolin 4'-O-sulfate (3) by the sulfation of quercetin, isoquercitrin (quercetin 3-O-glucoside) and

Design, synthesis and characterisation of mannosylated ovalbumin lipid core peptide self-adjuvanting vaccine delivery system.

Pavla Simerska et al.

Drug delivery and translational research, 4(3), 246-255 (2015-03-20)

Peptide-based vaccine delivery can be hampered by rapid peptidase activity and poor inherent immunogenicity. The self-adjuvanting lipid core peptide system (LCP) has been shown to confer improved stability and immunogenicity on peptide epitopes of group A Streptococcus, Chlamydia, hookworm, and

13C Tracking after 13CO2 Supply Revealed Diurnal Patterns of Wood Formation in Aspen.

Amir Mahboubi et al.

Plant physiology, 168(2), 478-489 (2015-05-02)

Wood of trees is formed from carbon assimilated in the photosynthetic tissues. Determining the temporal dynamics of carbon assimilation, subsequent transport into developing wood, and incorporation to cell walls would further our understanding of wood formation in particular and tree

Method development in quantitative NMR towards metrologically traceable organic certified reference materials used as (31)P qNMR standards.

Michael Weber et al.

Analytical and bioanalytical chemistry, 407(11), 3115-3123 (2014-11-25)

Quantitative nuclear magnetic resonance (qNMR) spectroscopy is employed by an increasing number of analytical and industrial laboratories for the assignment of content and quantitative determination of impurities. Within the last few years, it was demonstrated that (1)H qNMR can be

Dual evaluation of some novel 2-amino-substituted coumarinylthiazoles as anti-inflammatory-antimicrobial agents and their docking studies with COX-1/COX-2 active sites.

Navneet Chandak et al.

Journal of enzyme inhibition and medicinal chemistry, 29(4), 476-484 (2013-06-20)

Synthesis of total eighteen 2-amino-substituted 4-coumarinylthiazoles including sixteen new compounds (3a-o and 5b) bearing the benzenesulfonamide moiety is described in the present report. All the synthesized target compounds were examined for their in vivo anti-inflammatory (AI) activity and in vitro

Epsilon-caprolactone modified polyethylenimine for highly efficient antigen delivery and chemical exchange saturation transfer functional MR imaging.

Yan Tan et al.

Biomaterials, 56, 219-228 (2015-05-03)

Serious challenges remain in immunotherapy, such as to effectively deliver antigens and non-invasively monitor biological processes. Therefore, we aim to design a useful nanocarrier for enhancing antigen-specific immune response and performing functional molecular imaging guided immunotherapy. To achieve this goal

Discovery of novel Bcr-Abl inhibitors targeting myristoyl pocket and ATP site.

Jinyun Dong et al.

Bioorganic & medicinal chemistry, 22(24), 6876-6884 (2014-12-04)

Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were

Two new secondary metabolites from the marine-derived fungus Nigrospora sphaerica.

Qi-Hui Zhang et al.

Journal of Asian natural products research, 17(5), 497-503 (2015-03-24)

Two new secondary metabolites, (2S)-5-acetamidopentyl-2-hydroxypropanoate (1) and 2, 5, 7-trihydroxy-4-(3'-methylbut-2'-en-1'-yl) oxy-2H-naphtho [1, 8-b c] furan-9-one (2) were isolated from the marine-derived fungus Nigrospora sphaerica. The structures were established on the basis of their spectroscopic data, including 1D NMR and 2D

Permeation of Dopamine Sulfate through the Blood-Brain Barrier.

Tina Suominen et al.

PloS one, 10(7), e0133904-e0133904 (2015-07-25)

Dopamine sulfate (DA-3- and DA-4-S) have been determined in the human brain, but it is unclear whether they are locally formed in the central nervous system (CNS), or transported into the CNS from peripheral sources. In the current study, permeation

Cytotoxic activity of some novel sulfonamide derivatives.

Mostafa M Ghorab et al.

Acta poloniae pharmaceutica, 72(1), 79-87 (2015-04-09)

The versatile synthons 2-chloro-N-(4-sulfamoylphenyl)acetamides la,b were used as a key intermediates for the synthesis of sulfonamide derivatives with adamantyl 2, indene 3, morpholinophenyl 4, pipronyl 5, benzothiazole 6-8, pyrazole 9, thiadiazole 10,11, quinoline 12, isoquinoline 13, thiazoles 14-19, acrylamides 20-24

Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.

Srinivas Deekonda et al.

Bioorganic & medicinal chemistry letters, 26(1), 222-227 (2015-11-28)

N-Phenyl-N-(piperidin-2-ylmethyl)propionamide based bivalent ligands are unexplored for the design of opioid based ligands. Two series of hybrid molecules bearing N-phenyl-N-(piperidin-2-ylmethyl)propionamide derived small molecules conjugated with an enkephalin analogues with and without a linker (β-alanine) were designed and synthesized. Both bivalent

Synthesis of Unsaturated Polyester Resins from Various Bio-Derived Platform Molecules.

Thomas J Farmer et al.

International journal of molecular sciences, 16(7), 14912-14932 (2015-07-07)

Utilisation of bio-derived platform molecules in polymer synthesis has advantages which are, broadly, twofold; to digress from crude oil dependence of the polymer industry and secondly to reduce the environmental impact of the polymer synthesis through the inherent functionality of

Fast and effective photodynamic inactivation of multiresistant bacteria by cationic riboflavin derivatives.

Tim Maisch et al.

PloS one, 9(12), e111792-e111792 (2014-12-04)

Photodynamic inactivation of bacteria (PIB) proves to be an additional method to kill pathogenic bacteria. PIB requires photosensitizer molecules that effectively generate reactive oxygen species like singlet oxygen when exposed to visible light. To allow a broad application in medicine

Gum arabic-curcumin conjugate micelles with enhanced loading for curcumin delivery to hepatocarcinoma cells.

P R Sarika et al.

Carbohydrate polymers, 134, 167-174 (2015-10-03)

Curcumin is conjugated to gum arabic, a highly water soluble polysaccharide to enhance the solubility and stability of curcumin. Conjugation of curcumin to gum arabic is confirmed by (1)H NMR, fluorescence and UV spectroscopy studies. The conjugate self assembles to

Multivalent helix mimetics for PPI-inhibition.

Anna Barnard et al.

Organic & biomolecular chemistry, 13(1), 258-264 (2014-11-20)

The exploitation of multivalent ligands for the inhibition of protein-protein interactions has not yet been explored as a supramolecular design strategy. This is despite the fact that protein-protein interactions typically occur within the context of multi-protein complexes and frequently exploit

Experimental investigation on the soil sorption properties and hydrophobicity of polymethoxylated, polyhydroxylated diphenyl ethers and methoxylated-, hydroxylated-polychlorinated diphenyl ethers.

Xuesheng Zhang et al.

Chemosphere, 134, 84-90 (2015-04-29)

In the present study, twenty-six types of polymethoxylated diphenyl ethers (PMeODEs), twenty types of polyhydroxylated diphenyl ethers (PHODEs), seven types of methoxylated-polychlorinated diphenyl ethers (MeO-PCDEs) and seven types of hydroxylated-polychlorinated diphenyl ethers (HO-PCDEs) were synthesized. The logKow and logKoc values

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