Chemistry Central Journal

http://link.springer.com/journal/13065

List of Papers (Total 1,026)

Isolation, purification, structural analysis and coagulatory activity of water-soluble polysaccharides from Ligustrum lucidum Ait flowers

In this study, Ligustrum lucidum flowers as raw material, the extraction, isolation and coagulatory activity of polysaccharides were carried out for the first time. The crude polysaccharide was obtained by hot water extraction and ethanol precipitation, and preliminarily purified by Sevage method and D101 macroporous resin. Then the polysaccharide was further purified by DEAE-52 ...

Optimization of phenolics and flavonoids extraction conditions of Curcuma Zedoaria leaves using response surface methodology

This study focused on maximizing the extraction yield of total phenolics and flavonoids from Curcuma Zedoaria leaves as a function of time (80–120 min), temperature (60–80 °C) and ethanol concentration (70–90 v/v%). The data were subjected to response surface methodology (RSM) and the results showed that the polynomial equations for all models were significant, did not show lack of ...

Synthesis and biological evaluation of tricyclic matrinic derivatives as a class of novel anti-HCV agents

Background 12N-benzyl matrinic acid analogues had been identified to be a novel scaffold of anti-HCV agents with a specific mechanism, and the representative compound 1 demonstrated a moderate anti-HCV activity. The intensive structure–activity relationship of this kind of compounds is explored so as to obtain anti-HCV candidates with good druglike nature. Results Taking compound 1 ...

Synthesis, molecular docking and biological evaluation of bis-pyrimidine Schiff base derivatives

Background Heterocyclic pyrimidine nucleus, which is an essential base component of the genetic material of deoxyribonucleic acid, demonstrated various biological activities. A series of bis-pyrimidine Schiff bases were synthesized and screened for its antimicrobial and anticancer potentials. The molecular docking study was carried to find the interaction between active molecules ...

Phenolic compounds, flavonoids, lipids and antioxidant potential of apricot (Prunus armeniaca L.) pomace fermented by two filamentous fungal strains in solid state system

Background The use of agricultural and food by-products is an economical solution to industrial biotechnology. The apricot press residues are abounding by-products from juice industry which can be used as substrates in solid state fermentation process (SSF), thus allowing a liberation and increase of content from various biomolecules with high added value. Methods The evolutions of ...

Formation of amides: one-pot condensation of carboxylic acids and amines mediated by TiCl4

A general procedure for the synthesis of amides via the direct condensation of carboxylic acids and amines in the presence of TiCl4 is reported. The amidation reaction was performed in pyridine at 85 °C with a wide range of substrates providing the corresponding amide products in moderate to excellent yields and high purity. The reaction proceeds with low yields when both the ...

The development of an effective synthetic route of lesinurad (RDEA594)

Background Lesinurad is a novel selective uric acid salt transport protein 1 (URAT1) inhibitor which is approved in the USA for the treatment of gout. However, there are some shortcomings among the reported synthetic routes, such as expensive materials, environmental pollution and poor yield. Results In this study, an efficient, practical and environmentally-friendly synthetic ...

Synthesis, characterization, anti-ulcer action and molecular docking evaluation of novel benzimidazole-pyrazole hybrids

A series of six novel benzimidazole-pyrazole hybrid molecules was synthesized and characterized using elemental analysis (CHN) and spectroscopic methods (1HNMR, FT-IR). All the synthesized compounds were evaluated for their in vivo anti ulcerogenic activity using Albino rats (weighing 180–220 g). The interactions between the compounds and active site residues of H+/K+ ATPase were ...

Two phenolic antioxidants in Suoyang enhance viability of •OH-damaged mesenchymal stem cells: comparison and mechanistic chemistry

Background Suoyang originates from a psammophyte named Cynomorium songaricum Rupr and has been known as a phenolic-antioxidant-enriched traditional Chinese herbal medicine. The present study attempted to investigate the protective effect of phenolic antioxidants in Suoyang towards •OH-mediated MSCs and then further discusses the chemical mechanisms. Methods The lyophilized aqueous ...

Evaluation of antioxidant profile of various solvent extracts of Carissa opaca leaves: an edible plant

Background Carissa opaca leaves were conventionally recommended by local hakims in Pakistan for curing various human diseases including renal, hepatic and jaundice. In this work we arranged to study the antioxidant status of various fractions of C. opaca leaves through nine multifaceted assay systems. Methods Various fractions were prepared through solvent–solvent extraction ...

Comprehensive spectral identification of key intermediates to the final product of the chiral pool synthesis of radezolid

Radezolid (RAD, 12), biaryl oxazolidinone, was synthesised with small modifications according to the methods described in the literature. The pharmacological activity is observed only for (S)-enantiomer, therefore its synthesis is oriented towards obtaining a single isomer of required purity and desired optical configuration. The intermediate products of RAD synthesis were ...

Bis-pyrimidine acetamides: design, synthesis and biological evaluation

Background In the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents. On the other hand, bis-pyrimidines possess various types of biological activity. In view of this, in the present study we have designed and synthesized a new series of bis-pyrimidine ...

Surface bound radicals, char yield and particulate size from the burning of tobacco cigarette

Background Tobacco smoke is a toxic gas-phase cocktail consisting of a broad range of organics, and free radical intermediates. The formation of smoke from a burning cigarette depends on a series of mechanisms, including generation of products by pyrolysis and combustion, aerosol formation, and physical mass transfer processes. Methods The current study simulates the deposition of ...

One-step multicomponent synthesis of chiral oxazolinyl-zinc complexes

Background Typically, oxazolinyl metal complexes are synthesized in two steps, where the free ligand is prepared by the condensation reaction between a functionalized nitrile and an amino alcohol in the presence of a Lewis or Brønsted acid catalyst, followed by a further reaction with metal salts to obtain the corresponding metal complexes. Very often, the yield afforded by the ...

A comparative study of the metal binding behavior of alanine based bis-thiourea isomers

Two new symmetrical bis-thiourea, 2,2′-[{(terephthaloylbis(azanediyl)bis(carbonothioyl) bis(azanediyl)}dipropanoic acid] (1A) and 3,3′-[{(terephthaloylbis(azanediyl)bis (carbonothioyl)bis(azanediyl)} dipropanoic acid] (1B) were synthesized by the reaction of terephthaloyl chloride with α- and β-alanine in good yields. Their binding properties were investigated with various metal ...

Directed Assembly Network phase three launch: a round-up of success to date and strategy for the future

To showcase the Networks’ success during phase two (2012–2016), and to set out the strategy for phase three (2017–2019), the Directed Assembly Network held a meeting at the Royal Society in London, United Kingdom on 14 and 15 December 2016. Seventy Network members from both industry and academia attended the event. The meeting, which was used as a springboard to launch and ...

Comparison of various techniques for the extraction of umbelliferone and herniarin in Matricaria chamomilla processing fractions

Chamomile, a well-known medicinal plant, is a rich source of bioactive compounds, among which two coumarin derivatives, umbelliferone and herniarin, are often found in its extracts. Chamomile extracts have found a different uses in cosmetic industry, as well as umbelliferone itself, which is, due to its strong absorption of UV light, usually added to sunscreens, while herniarin ...

Regioselective semi-synthesis of 6-isomers of 5,8-O-dimethyl ether of shikonin derivatives via an ‘intramolecular ring-closing/ring-opening’ strategy as potent anticancer agents

Synthesis of 6-isomer of 5,8-O-dimethyl ether of shikonin (13), a promising anticancer scaffold, always remains a huge challenge. Herein a key intermediate for 13, 2-(1-hydroxyl-4-methyl-3-pentenyl)-1,4,5,8-tetramethoxynaphthalene (10), was obtained on the large-scale synthesis. A ring-closing/ring-opening strategy was applied to avoid the undesired reactivity posed by the side ...

Antimicrobial activity of thiophene derivatives derived from ethyl (E)-5-(3-(dimethylamino)acryloyl)-4-methyl-2-(phenylamino)thiophene-3-carboxylate

Background The thiophene nucleus has been recognized as an important entity in the synthesis of heterocyclic compounds with promising pharmacological characteristics. Results A number of new heterocyclic compounds incorporating thiophene species have been prepared from the titled enaminone via the reaction with different nucleophiles and electrophiles. The structure elucidation of ...

Ultra-high resolution X-ray structures of two forms of human recombinant insulin at 100 K

The crystal structure of a commercially available form of human recombinant (HR) insulin, Insugen (I), used in the treatment of diabetes has been determined to 0.92 Å resolution using low temperature, 100 K, synchrotron X-ray data collected at 16,000 keV (λ = 0.77 Å). Refinement carried out with anisotropic displacement parameters, removal of main-chain stereochemical restraints, ...

Structural optimization and evaluation of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole derivatives as potential VEGFR-2/PDGFRβ inhibitors

Background Tumor angiogenesis, essential for tumor growth and metastasis, is tightly regulated by VEGF/VEGFR and PDGF/PDGFR pathways, and therefore blocking those pathways is a promising therapeutic target. Compared to sunitinib, the C(5)-Br derivative of 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole has significantly greater in vitro activities against VEGFR-2, PDGFRβ, ...

Structural effects on kinetics and a mechanistic investigation of the reaction between DMAD and N–H heterocyclic compound in the presence of triphenylarsine: spectrophotometry approach

Kinetics and a mechanistic investigation of the reaction between dimethyl acetylenedicarboxcylate (DMAD) and saccharin (N–H heterocyclic compound) has been spectrally studied in methanol environment in the presence of triphenylarsine (TPA) as a catalyst. Previously, in a similar reaction, triphenylphosphine (TTP) (instead of triphenylarsine) has been employed as a third reactant ...

Novel drug targets for Mycobacterium tuberculosis: 2-heterostyrylbenzimidazoles as inhibitors of cell wall protein synthesis

Background Multi drug-resistant and mycobacterial infections are a major public health challenge, leading to high mortality and socioeconomic burdens through worldwide. Novel therapeutics are necessary to treat the drug resistant strains, since no new chemical entities are emerged in the last four decades for the treatment of TB. Findings A series of novel ...