Chemistry Central Journal

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

List of Papers (Total 1,111)

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, PDGFR...

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 2...

Fingerprint analysis of Resina Draconis by ultra-performance liquid chromatography

Background Resina Draconis, a bright red resin derived from Dracaena cochinchinensis, is a traditional medicine used in China. To improve its quality control approach, an ultra-performance liquid chromatography (UPLC) fingerprint method was developed for rapidly evaluating the quality of Resina Draconis. Methods The precision, repeatability and stability of the proposed UPLC...

RD-Metabolizer: an integrated and reaction types extensive approach to predict metabolic sites and metabolites of drug-like molecules

Background Experimental approaches for determining the metabolic properties of the drug candidates are usually expensive, time-consuming and labor intensive. There is a great deal of interest in developing computational methods to accurately and efficiently predict the metabolic decomposition of drug-like molecules, which can provide decisive support and guidance for...

One pot synthesis, antimicrobial and antioxidant activities of fused uracils: pyrimidodiazepines, lumazines, triazolouracil and xanthines

Background Uracil derivatives have a great attraction because they play an important role in pharmacological activities. Pyrimidodiazepines, lumazines, triazolopyrimidines and xanthines have significant wide spectrum activities including anticancer, antiviral as well as antimicrobial activities. Results A newly synthesized compounds pyrimido[4,5-b][1, 4]diazepines 5a–e, 6a–d...

Comparative study of phenolic compounds, vitamin E, and fatty acids compositional profiles in black seed-coated soybeans (Glycine Max (L.) Merrill) depending on pickling period in brewed vinegar

BackgroundPickled soybeans or vinegar beans have long been used as a folk remedy and also a supplemental nutritional source in Korea. In general the pickling process in vinegar improves the digestibility of soybeans as well as increases the availability of various (non-)nutrients in soybeans. However, detailed information about the changes in functional substances such as (poly...

Using crystallography, topology and graph set analysis for the description of the hydrogen bond network of triamterene: a rational approach to solid form selection

This study has demonstrated the use of crystallography, topology and graph set analysis in the description and classification of the complex hydrogen bonded network of triamterene. The aim is to give a brief overview of the methodology used to discuss the crystal structure of triamterene with a view to extending the study to include the solvates, cocrystals and salts of this...

The mechanism for enhanced oxidation degradation of dioxin-like PCBs (PCB-77) in the atmosphere by the solvation effect

The reaction pathways of PCB-77 in the atmosphere with ·OH, O2, NO x , and 1O2 were inferred based on density functional theory calculations with the 6-31G* basis set. The structures the reactants, transition states, intermediates, and products were optimized. The energy barriers and reaction heats were obtained to determine the energetically favorable reaction pathways. To study...

A review of traditional pharmacological uses, phytochemistry, and pharmacological activities of Tribulus terrestris

Tribulus terrestris L. (TT) is an annual plant of the family Zygophyllaceae that has been used for generations to energize, vitalize, and improve sexual function and physical performance in men. The fruits and roots of TT have been used as a folk medicine for thousands of years in China, India, Sudan, and Pakistan. Numerous bioactive phytochemicals, such as saponins and...

A validated stability-indicating HPLC method for determination of brimonidine tartrate in BRI/PHEMA drug delivery systems

Background A simple, rapid and accurate stability-indicating reverse phase high performance liquid chromatography (RP-HPLC) was developed and validated for the determination of brimonidine tartrate in brimonidine tartrate/poly(2-hydroxyethyl methacrylate) (BRI/PHEMA) drug delivery contact lenses and pharmaceutical formulations. Results Optimum chromatographic conditions for...

Comparative studies on phenolic profiles, antioxidant capacities and carotenoid contents of red goji berry (Lycium barbarum) and black goji berry (Lycium ruthenicum)

Background The study on phytochemical difference between red and black goji berry is limited. Methods Antioxidant activities and phenolic profiles in terms of total phenol content, total flavonoid contents, condensed tannin content, monomeric anthocyanin content, and total carotenoid content of red goji berry (Lycium barbarum) and black goji berry (L. ruthenicum) were compared...

Selective synthesis of Fe3O4Au x Ag y nanomaterials and their potential applications in catalysis and nanomedicine

In these recent years, magnetite (Fe3O4) has witnessed a growing interest in the scientific community as a potential material in various fields of application namely in catalysis, biosensing, hyperthermia treatments, magnetic resonance imaging (MRI) contrast agents and drug delivery. Their unique properties such as metal–insulator phase transitions, superconductivity, low Curie...

Antiproliferative and apoptotic effects of black turtle bean extracts on human breast cancer cell line through extrinsic and intrinsic pathway

The black turtle bean (BTB) is most widely consumed legume all over the world having anticancer activity. The aim of the study was to analyse the apoptotic effects of BTB extracts on human breast cancer cell lines. Plant extract was prepared by homogenization and centrifugation. The cytotoxic effects of BTB was evaluated by MTT assay and their apoptotic effects were characterized...

Utility of 2-thioxo-pyrido[2,3-d]pyrimidinone in synthesis of pyridopyrimido[2,1-b][1,3,5]-thiadiazinones and pyridopyrimido[2,1-b][1,3]thiazinones as antimicrobial agents

Background Pyridopyrimidines are of current interest because of their extensive variety of biological and pharmacological activities. Results A series of pyrido[2′,3′:4,5]pyrimido[2,1-b][1,3,5]thiadiazinones was obtained by aminomethylation of pyridopyrimidinethione with formaldehyde solution (37%) and different primary aromatic amines. Another series of pyrido[2′,3:4,5]pyrimido...

Hemostatic chemical constituents from natural medicine Toddalia asiatica root bark by LC-ESI Q-TOF MSE

Background Toddalia asiatica root bark as an effective hemostatic natural medicine or Chinese materia medica was applied in China for long history, its complex drug action mechanisms and unclear substance basis have been constraining the development of this drug. Results An intelligentized strategy by LC-ESI Q-TOF MSE was presented in this study for rapid identification of...

Effects of temperature, time, and solvent ratio on the extraction of phenolic compounds and the anti-radical activity of Clinacanthus nutans Lindau leaves by response surface methodology

Background Clinacanthus nutans Lindau is a well-known plant, native to tropical Asian countries. Reports on this plant that is rich in phenolic compounds have focused on its therapeutic anti-inflammatory, anti-herpes simplex, antioxidant, and anti-cancer characteristics. In this paper, the influence of the extraction parameters—temperatures (60–80 °C), times (80–120 min), and...

Synthesis of some new pyrazolo[1,5-a]pyrimidine, pyrazolo[5,1-c]triazine, 1,3,4-thiadiazole and pyridine derivatives containing 1,2,3-triazole moiety

Background Pyrazolo[1,5-a]pyrimidines are purine analogues. They have beneficial properties as antimetabolites in purine biochemical reactions. This division compounds have attracted wide pharmaceutical interest because of their antitrypanosomal activity. Results The present work depicts an effective synthesis convention of pyrazolo[1,5-a]pyrimidines, pyrazolo[5,1-c]triazines...

Design, synthesis and antimicrobial evaluation of pyrimidin-2-ol/thiol/amine analogues

Background Pyrimidine is an aromatic heterocyclic moiety containing nitrogen atom at 1st and 3rd positions and play an important role to forms the central core for different necessity of biological active compounds, from this facts, we have designed and synthesized a new class of pyrimidin-2-ol/thiol/amine derivatives and screened for its in vitro antimicrobial activity. Results...

Synthesis, characterization, X-ray structure, computational studies, and bioassay of novel compounds combining thiophene and benzimidazole or 1,2,4-triazole moieties

Background Due to their interesting and versatile biological activity, thiophene-containing compounds have attracted the attention of both chemists and medicinal chemists. Some of these compounds have anticancer, antibacterial, antiviral, and antioxidant activity. In addition, the thiophene nucleus has been used in the synthesis of a variety of heterocyclic compounds. Results In...

Synthesis and insecticidal activity of diacylhydrazine derivatives containing a 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole scaffold

Background The diacylhydrazine derivatives have attracted considerable attention in recently years due to their simple structure, low toxicity, and high insecticidal selectivity. As well as 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole is an important scaffold in many insecticidal molecules. In an effort to discover new molecules with good insecticidal activity, a series of...

Gadolinium-based layered double hydroxide and graphene oxide nano-carriers for magnetic resonance imaging and drug delivery

Gadolinium (Gd)-based contrasts remain one of the most accepted contrast agents for magnetic resonance imaging, which is among the world most recognized noninvasive techniques employed in clinical diagnosis of patients. At ionic state, Gd is considered toxic but less toxic in chelate form. A variety of nano-carriers, including gadolinium oxide (Gd2O3) nanoparticles have been used...

Liquid chromatography tandem mass spectrometry method for the quantification of vandetanib in human plasma and rat liver microsomes matrices: metabolic stability investigation

Vandetanib (VNT) is a new oral tyrosine kinase inhibitor that acts mainly by inhibiting vascular endothelial growth factor receptor (VEGFR). Fast, specific, sensitive and validated LC–MS/MS was established for the determination of VNT in two various matrices including rat liver microsomes (RLMs) and human plasma. This method was applied in metabolic stability investigation of VNT...