Chemistry Central Journal

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

List of Papers (Total 1,121)

LC–MS/MS method for the quantification of masitinib in RLMs matrix and rat urine: application to metabolic stability and excretion rate

Masitinib (MST) is a selective tyrosine kinase inhibitor. Validated liquid chromatography tandem mass spectrometric method (LC–MS/MS) was developed for the quantification of MST in rat liver microsomes (RLMs) matrix. The developed method was applied to metabolic stability and excretion rate studies. Reversed phase liquid chromatography was used for resolution of MST and bosutinib...

Design, synthesis and biological evaluation of antimalarial activity of new derivatives of 2,4,6-s-triazine

Dihydrofolate reductase (DHFR) is an important enzyme for de novo synthesis of nucleotides in Plasmodium falciparum and it is essential for cell proliferation. DHFR is a well known antimalarial target for drugs like cycloguanil and pyrimethamine which target its inhibition for their pharmacological actions. However, the clinical efficacies of these antimalarial drugs have been...

Comprehensive survey of radionuclides in contemporary smokeless tobacco products

There is considerable interest in the chemical composition of smokeless tobacco products (STPs), owing to health concerns associated with their use. Previous studies have documented levels of 210Po, 210Pb and uranium in STP samples. Here, the levels of 13 α-particle and 15 β-radiation emitting radionuclides have been measured in a broad and representative range of contemporary...

Comparative efficacy of locally isolated fungal strains for Pb(II) removal and recovery from water

The present investigation aimed to study and compare the efficiency of non-viable fungal isolates to remove divalent lead (Pb(II)) from aqueous streams. The selected fungal isolates showed identity with Aspergillus caespitosus, Aureobasidium sp. RBSS-303 and Aspergillus flavus HF5 as confirmed using gene sequencing of ITS regions of the ribosomal DNA (rDNA). The obtained...

Study of binding interaction of rivaroxaban with bovine serum albumin using multi-spectroscopic and molecular docking approach

Background Rivaroxaban is a direct inhibitor of coagulation factor Xa and is used for venous thromboembolic disorders. The rivaroxaban interaction with BSA was studied to understand its PK and PD (pharmacokinetics and pharmacokinetics) properties. Multi-spectroscopic studies were used to study the interaction which included UV spectrophotometric, spectrofluorometric and three...

Development of new analytical methods for the determination of caffeine content in aqueous solution of green coffee beans

Background This study was conducted to develop fast and cost effective methods for the determination of caffeine in green coffee beans. In the present work direct determination of caffeine in aqueous solution of green coffee bean was performed using FT-IR-ATR and fluorescence spectrophotometry. Caffeine was also directly determined in dimethylformamide solution using NIR...

Synthesis, structure and toxicity evaluation of ethanolamine nitro/chloronitrobenzoates: a combined experimental and theoretical study

Background Nitroaromatic and chloronitroaromatic compounds have been a subject of great interest in industry and recently in medical-pharmaceutic field. 2-Chloro-4-nitro/2-chloro-5-nitrobenzoic acids and 4-nitrobenzoic acid are promising new agents for the treatment of main infectious killing diseases in the world: immunodeficiency diseases and tuberculosis. Results New...

Investigating and characterizing the binding activity of the immobilized calmodulin to calmodulin-dependent protein kinase I binding domain with atomic force microscopy

Protein–protein interactions are responsible for many biological processes, and the study of how proteins undergo a conformational change induced by other proteins in the immobilized state can help us to understand a protein’s function and behavior, empower the current knowledge on molecular etiology of disease, as well as the discovery of putative protein targets of therapeutic...

An improved solvent-free synthesis of flunixin and 2-(arylamino) nicotinic acid derivatives using boric acid as catalyst

A simple solvent-free protocol for the preparation of flunixin, a potent non-narcotic, non-steroidal anti-inflammatory drugs is reported using boric acid as catalyst. Its salt, flunixin meglumine are then prepared under reflux in EtOH. This sustainable method are then extended for the synthesis of a series of 2-(arylamino) nicotinic acid derivatives. The present protocol combines...

Structure-dependent optoelectronic properties of perylene, di-indenoperylene (DIP) isolated molecule and DIP molecular crystal

Theoretical simulations were designed by first principles approach of density functional theory to investigate the structural and optoelectronic properties of different structural classes of perylene; isolated perylene, diindeno[1,2,3-cd:1′,2′,3′-lm]perylene (DIP) molecule and DIP molecular crystal. The presence of molecular interactions in DIP crystal proved its structure...

Synthesis, anti-angiogenic and DNA cleavage studies of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives

A series of novel N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives 10(a–f), 12(a–c) and 14(a–c) were synthesized and characterized by FTIR, 1H-NMR, mass spectral and elemental analysis. The efficacy of these derivatives to inhibit in vivo angiogenesis was evaluated using chick chorioallantoic membrane (CAM) model and their DNA...

Correction to: Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c] pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives

After the publication of this work [1] it was noticed that on page 3 of the article beginning in the paragraph—‘Hydrazide 14 is used as a key producer…’ the compound—“Not ethyl-N′-5-amino-1,3-diphenyl-1H-thieno[3,2-c]pyrazole-6-carbonylformohydrazonate” should be deleted. Also on page 10 of the PDF beginning in paragraph—‘Synthesis of 5-amino-…’ the compound—“Not ethyl-N′-5-amino...

Determination of lesinurad in rat plasma by a UHPLC–MS/MS assay

Lesinurad is an oral inhibitor of urate-anion exchanger transporter 1 and has been approved by the US Food and Drug Administration for combination therapy with a xanthine oxidase inhibitor for the treatment of hyperuricemia associated with refractory gout. In the present study, a sensitive and specific ultra high-performance liquid chromatography with tandem mass spectrometry...

Electrochemical behavior and in-vitro antimicrobial screening of some thienylazoaryls dyes

Background A series of recently reported phenolic azo dyes 7a–e were prepared by coupling the thienyl diazonium sulfate of 3-Amino-4H-benzo[f]thieno[3,4-c](2H)chromen-4-one with selected diversely substituted phenolic and naphtholic derivatives. These compounds were evaluated for their antibacterial and antifungal activities. Furthermore their voltammetric behavior was compared...

Design, synthesis, in silico and in vitro antimicrobial screenings of novel 1,2,4-triazoles carrying 1,2,3-triazole scaffold with lipophilic side chain tether

Background 1,2,4-Triazoles and 1,2,3-triazoles have gained significant importance in medicinal chemistry. Results This study describes a green, efficient and quick solvent free click synthesis of new 1,2,3-triazole-4,5-diesters carrying a lipophilic side chain via 1,3-dipolar cycloaddition of diethylacetylene dicarboxylate with different surfactant azides. Further structural...

Phenolic constituents from Alisma plantago-aquatica Linnaeus and their anti-chronic prostatitis activity

Background The plant Alisma plantago-aquatica Linnaeus, which is widely distributed in southwest of China, is the main material of traditional Chinese medicine “Zexie”. It was used as folk medicine for immune-modulation, anti-tumor, anti-inflammatory and antibacterial. Previous chemical studies on A. plantago-aquatica reported the identification of triterpenes, diterpenes...

Polysaccharides from Dolichos biflorus Linn and Trachyspermum ammi Linn seeds: isolation, characterization and remarkable antimicrobial activity

Polysaccharides are structurally complex and essential constituents of life, and therefore, studies directed to these kinds of molecules have received scientific attention. Despite an easy availability of Dolichos biflorus Linn and Trachyspermum ammi (Linn) seeds isolation, characterization and antimicrobial studies of polysaccharides derived from these two natural sources have...

Study on the interaction of paeoniflorin with human serum albumin (HSA) by spectroscopic and molecular docking techniques

The interaction of paeoniflorin with human serum albumin (HSA) was investigated using fluorescence, UV–vis absorption, circular dichroism (CD) spectra and molecular docking techniques under simulative physiological conditions. The results clarified that the fluorescence quenching of HSA by paeoniflorin was a static quenching process and energy transfer as a result of a newly...

Design, synthesis, conformational and molecular docking study of some novel acyl hydrazone based molecular hybrids as antimalarial and antimicrobial agents

BackgroundAcyl hydrazones are an important class of heterocyclic compounds promising pharmacological characteristics. Malaria is a life-threatening mosquito-borne blood disease caused by a plasmodium parasite. In some places, malaria can be treated and controlled with early diagnosis. However, some countries lack the resources to do this effectively.ResultsThe present work...

Simultaneous determination of brazilin and protosappanin B in Caesalpinia sappan by ionic-liquid dispersive liquid-phase microextraction method combined with HPLC

The conditions of heating, ionic liquid-based ultrasonic-assisted extraction combined with reverse-phase high performance liquid chromatography were optimized to simultaneously isolate and determinate brazilin and protosappanin B in Caesalpinia sappan. Ionic liquids, including [BMIM]Br, [BMIM]BF4, [BMIM]PF6 and [HMIM]PF6, were selected as extraction solvents while methanol...

Antimicrobial and antioxidant potential of different solvent extracts of the medicinal plant Geum urbanum L.

Many Geum species are known to be rich in biologically active compounds and therefore could be a source of new natural products with pharmacological potential. The medicinal plant Geum urbanum L. is widespread in Bulgaria and has been used in folk medicine. In the present study, the methanol extracts of the roots and aerial parts of G. urbanum and their fractions (petroleum ether...

Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives

Background Some novel substituted pyrazolone, pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidinone, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives have been reported to possess various pharmacological activities like antimicrobial, antitumor and anti-inflammatory. Results A novel series of azoles and...

Aromatherapy: composition of the gaseous phase at equilibrium with liquid bergamot essential oil

This work compares the composition at different temperatures of gaseous phase of bergamot essential oil at equilibrium with the liquid phase. A new GC–MS methodology to determine quantitatively the volatile aroma compounds was developed. The adopted methodology involved the direct injection of headspace gas into injection port of GC–MS system and of known amounts of the...

Antioxidant and antiproliferative activity of blue corn and tortilla from native maize

Background Blue corn is a cereal rich in phenolic compounds used to make blue tortillas. Tortillas are an important part of the Mexican diet. Blue corn and tortilla represent an important source of the natural antioxidants anthocyanins. However, studies on their biological activity on cancer cell lines are limited. The goal of this study was to evaluate the antioxidant and...

Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

A series of diamides derivatives containing nicotinamide unit were designed, synthesized and evaluated for their potential cytotoxic activities against human cancer cell lines. All the synthesized compounds were characterized using spectroscopic methods mainly including 1H NMR, 13C NMR and MS. The bio-evaluation results indicated that some of the obtained compounds (such as 4d...