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Chemistry Central Journal

Yiketel Adege Chekol, Zelalem Yibralign Desta
BACKGROUND: The extracts from the leaves of Otostegia integrifolia have been reported to show phytochemical analysis, total flavonoid content, antioxidant and antibacterial activities. RESULTS: Our results revealed that the total flavonoid content of methanol and ethyl acetate extracts is 416.5 + 0.288 and 248.9 + 0.872 mgAAE/100 g respectively. The two extracts also showed good antioxidant activity as well as weak to moderate antibacterial activity against some bacteria...
May 18, 2018: Chemistry Central Journal
Humaira Yasmeen Gondal, Zain Maqsood Cheema, Javid Hussain Zaidi, Sammer Yousuf, M Iqbal Choudhary
An efficient one pot method for the synthesis of α-alkoxymethylphosphonium iodides is developed by using PPh3 /I2 combination at room temperature. Reaction conditions are found general to synthesize wide range of structurally variant alkoxymethylphosphonium iodides in high yield (70-91%). These new functionalized phosphonium salts are further used in stereoselective synthesis of vinyl ethers as well as in carbon homologation of aldehydes.
May 17, 2018: Chemistry Central Journal
Adnan A Kadi, Sawsan M Amer, Hany W Darwish, Mohamed W Attwa
Masitinib (MST) is an orally administered drug that targets mast cells and macrophages, important cells for immunity, by inhibiting a limited number of tyrosine kinases. It is currently registered in Europe and USA for the treatment of mast cell tumors in dogs. AB Science announced that the European Medicines Agency has accepted a conditional marketing authorization application for MST to treat amyotrophic lateral sclerosis. In our work, we focused on studying in vivo metabolism of MST in Sprague-Dawley rats...
May 15, 2018: Chemistry Central Journal
Hagos Yisak, Mesfin Redi-Abshiro, Bhagwan Singh Chandravanshi
BACKGROUND: There is no fluorescence spectroscopic method for the determination of trigonelline and theobromine in green coffee beans. Therefore, the objective of this study was to develop a new fluorescence spectroscopic method to determine the alkaloids simultaneously in the aqueous extract of green coffee beans. RESULTS: The calibration curves were linear in the range 2-6, 1-6, 1-5 mg/L for caffeine, theobromine and trigonelline, respectively, with R2  ≥ 0...
May 11, 2018: Chemistry Central Journal
Songsong Zhao, Xinjia Yan, Ying Zhao, Jing Wen, Zhenzhen Zhao, Hongwei Liu
BACKGROUND: Radix Glycyrrhizae is the rhizome of Glycyrrhiza inflata Bat., Glycyrrhiza uralensis Fisch. or Glycyrrhiza glabra L. The present paper describes the isolation and the structural elucidation of three new dihydroisocoumarins obtained from the 70% EtOH extract of Radix Glycyrrhizae. And the cytotoxic activities of these new compounds were also evaluated using four cell lines, subsequently. RESULTS: A pair of new dihydroisocoumarin epimers ((3R,4S)-4,8-dihydroxy-3-methyl-1-oxoisochroman-5-yl)methyl acetate (1) and ((3R,4R)-4,8-dihydroxy-3-methyl-1-oxoisochroman-5-yl)methyl acetate (2) along with a new dihydroisocoumarin (3R,4R)-4,8-dihydroxy-3,5-dimethylisochroman-1-one (3) were isolated from Radix Glycyrrhizae...
May 11, 2018: Chemistry Central Journal
Yahia N Mabkhot, Mohammed M Alharbi, Salim S Al-Showiman, Hazem A Ghabbour, Nabila A Kheder, Saied M Soliman, Wolfgang Frey
BACKGROUND: The synthesis of new thiazole derivatives is very important because of their diverse biological activities. Also , many drugs containing thiazole ring in their skeletons are available in the market such as Abafungin, Acotiamide, Alagebrium, Amiphenazole, Brecanavir, Carumonam, Cefepime, and Cefmatilen. RESULTS: Ethyl cyanoacetate reacted with phenylisothiocyanate, chloroacetone, in two different basic mediums to afford the thiazole derivative 6, which reacted with dimethylformamide- dimethyl acetal in the presence of DMF to afford the unexpected thiazole derivative 11...
May 11, 2018: Chemistry Central Journal
Krzysztof Marciniec, Rafał Kurczab, Maria Książek, Ewa Bębenek, Elwira Chrobak, Grzegorz Satała, Andrzej J Bojarski, Joachim Kusz, Paweł Zajdel
A series of azinesulfonamide derivatives of long-chain arylpiperazines with variable-length alkylene spacers between sulfonamide and 4-arylpiperazine moiety is designed, synthesized, and biologically evaluated. In vitro methods are used to determine their affinity for serotonin 5-HT1A , 5-HT6 , 5-HT7 , and dopamine D2 receptors. X-ray analysis, two-dimensional NMR conformational studies, and docking into the 5-HT1A and 5-HT7 receptor models are then conducted to investigate the conformational preferences of selected serotonin receptor ligands in different environments...
May 11, 2018: Chemistry Central Journal
Si-Hong Ou-Yang, Tao Jiang, Lin Zhu, Tao Yi
Dioscorea nipponica Makino is a perennial twining herbs belonging to the family Dioscoreaceae, which is mainly distributed in the northeastern, northern, eastern and central regions of China. Traditionally, the rhizome of this herb has been commonly used by Miao and Meng ethnic groups of China to treat rheumatoid arthritis, pain in the legs and lumbar area, Kashin Beck disease, bruises, sprains, chronic bronchitis, cough and asthma. Modern pharmacological studies have discovered that this herb possesses anti-tumor, anti-inflammatory, anti-diuretic, analgesic, anti-tussive, panting-calming and phlegm-dispelling activities, along with enhancing immune function and improving cardiovascular health...
May 11, 2018: Chemistry Central Journal
Sompit Wanwong, Piyachai Khomein, S Thayumanavan
A series of D-A dyads and D-A-D triads molecular systems based on triphenylamine and 9-ethyl-carbarzole as donor (D) and BODIPY as acceptor (A) has been designed and synthesized. The optoelectronic properties including optical, electrochemical, and charge carrier mobility of these molecules have been investigated. We found that the D-A-D triads exhibited broader absorption, raising the HOMO energy levels and increase hole carrier mobilities. Analysis surface morphology revealed that BODIPY containing carbazole demonstrated smooth film and no macro phase aggregation was observed upon thermal annealing...
May 11, 2018: Chemistry Central Journal
Pablo Luis B Figueiredo, Renan C Silva, Joyce Kelly R da Silva, Chieno Suemitsu, Rosa Helena V Mourão, José Guilherme S Maia
BACKGROUND: Psidium guineense, known as Araçá, is a Brazilian botanical resource with commercial application perspectives, based on the functional elements of its fruits and due to the use of its leaves as an anti-inflammatory and antibacterial agent. The essential oils of leaves of twelve specimens of Araçá were analyzed by GC and GC-MS to identify their volatile constituents and associate them with the biological activities reputed to the plant. RESULTS: In a total of 157 identified compounds, limonene, α-pinene, β-caryophyllene, epi-β-bisabolol, caryophyllene oxide, β-bisabolene, α-copaene, myrcene, muurola-4,10(14)-dien-1-β-ol, β-bisabolol, and ar-curcumene were the primary components in descending order up to 5%...
May 10, 2018: Chemistry Central Journal
Arão Cardoso Viana, Ingrid Graça Ramos, Edeilza Lopes Dos Santos, Artur José Santos Mascarenhas, Marcos Dos Santos Lima, Antônio Euzébio Goulart Sant'Ana, Janice Izabel Druzian
A fast method for the identification and stability evaluation of the aggregation pheromone rhynchophorol, which is the main substance used for chemical communication by the beetle Rhynchophorus palmarum L., was validated. In addition, the technique was applied to the evaluation of two inorganic matrices, with the objective of using them as controlled-release devices. The analytical method showed good linearity (R2  = 0.9978), precision (CV% < 1.79), recovery (84-105%) and limits of detection (0.2 mg mL-1 ) and quantification (0...
May 10, 2018: Chemistry Central Journal
S Andrade-Ochoa, J Correa-Basurto, L M Rodríguez-Valdez, L E Sánchez-Torres, B Nogueda-Torres, G V Nevárez-Moorillón
BACKGROUND: In order to develop new larvicidal agents derived from phytochemicals, the larvicidal activity of fifty molecules that are constituent of essential oils was evaluated against Culex quinquefasciatus Say. Terpenes, terpenoids and phenylpropanoids molecules were included in the in vitro evaluation, and QSAR models using genetic algorithms were built to identify molecular and structural properties of biological interest. Further, to obtain structural details on the possible mechanism of action, selected compounds were submitted to docking studies on sterol carrier protein-2 (SCP-2) as possible target...
May 10, 2018: Chemistry Central Journal
Heba A Elhady, Refat El-Sayed, Hamedah S Al-Nathali
A novel series of substituted 2-thiohydantoin incorporated with benzoimidazole, pyrazole, triazole and/or benzoxazole moieties has been synthesized using (E)-3-[1-(4-bromophenyl)ethylideneamino]-2-thioxoimidazolidin-4-one 1 as the key starting material. The key material 1 also, reacted with an acetic anhydride, aromatic aldehydes, secondary amines, formaldehyde and triethyl orthoformate to give the corresponding acetyl, chalcone, Mannich bases and ethoxymethylene derivatives, respectively. The structures of the novel compounds were confirmed by spectral data and elemental analysis...
May 9, 2018: Chemistry Central Journal
Ayman M S Youssef, Ahmed M Fouda, Rasha M Faty
BACKGROUND AND OBJECTIVE: A series of thiazolopyrimidine derivatives have been synthesized via multicomponent reaction and tested for biological activities. This research aims to develop a new synthetic method of poly fused pyrimidines under microwave irradiation. 6-Amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitriles reacted with bromomalono-nitrile to give 3,7-diamino-5-aryl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarbonitrile more willingly than the isomeric 7H-thiazolo[3,2-a]pyrimidines...
May 5, 2018: Chemistry Central Journal
Komal Rizwan, Muhammad Zubair, Nasir Rasool, Tariq Mahmood, Khurshid Ayub, Noorjahan Banu Alitheen, Muhammad Nazirul Mubin Aziz, Muhammad Nadeem Akhtar, Faiz-Ul-Hassan Nasim, Snober Mona Bukhary, Viqar Uddin Ahmad, Mubeen Rani
Thiophene derivatives have shown versatile pharmacological activities. The Suzuki reaction proved a convenient method for C-C bond formations in organic molecules. In the present research work novel derivatives of 2,5-dibromo-3-methylthiophene (3a-k and 3l-p) has been synthesized, via Suzuki coupling reaction in low to moderate yields. A wide range of functional groups were well tolerated in reaction. Density functional theory investigations on all synthesized derivatives (3a-3p) were performed in order to explore the structural properties...
May 4, 2018: Chemistry Central Journal
Qishu Jiao, Rufeng Wang, Yanyan Jiang, Bin Liu
Traditional Chinese medicine (TCM), as a unique form of natural medicine, has been used in Chinese traditional therapeutic systems over two thousand years. Active components in Chinese herbal medicine are the material basis for the prevention and treatment of diseases. Research on drug-protein binding is one of the important contents in the study of early stage clinical pharmacokinetics of drugs. Plasma protein binding study has far-reaching influence on the pharmacokinetics and pharmacodynamics of drugs and helps to understand the basic rule of drug effects...
May 4, 2018: Chemistry Central Journal
Haitham Alrabiah, Adnan A Kadi, Mohamed W Attwa, Gamal A E Mostafa
PURPOSE: To develop and validate a bio-analytical HPLC-MS/MS method for the determination of conivaptan (CVA) an arginine-vasopressin receptor blocker in human plasma and in rat liver microsomes (RLMs). METHODS: Analytes were separated on a reversed phase C18 column (50 mm × 2.1 mm, 1.8 μm). The mobile phase was a mixture of acetonitrile and 10 mM ammonium formate (40:60 v/v, pH 4.0) and was pumped isocratically for 4 min at a flow rate of 0.2 ml/min...
May 2, 2018: Chemistry Central Journal
Mirza Nadeem Ahmad, Fakher Rafique, Faisal Nawaz, Tahir Farooq, Muhammad Naveed Anjum, Tajamal Hussain, Sajjad Hassan, Madeeha Batool, Hamad Khalid, Khurram Shehzad
Electrically conductive polyorthochloroaniline/chromium nanocomposites (POC/Cr NCs) were prepared by in situ chemical oxidative polymerization of orthochloroaniline in the presence of Cr nanoparticles (Cr NPs). The load percentage of Cr nanofiller was varied in POC matrix to investigate the effect of Cr nanoparticles on the properties of the nanocomposites. The composition, structure, and morphology of POC and its composites were examined by Scanning electron microscopy, Fourier transform infrared spectroscopy, and UV-visible spectroscopic analysis...
April 26, 2018: Chemistry Central Journal
Li Zhang, Tiehu Li, Lei Huang, Zhengqin Ye, Zhongbin Ye, Xin Yan, Lili Li, Qiang Deng, Gang Chen, Jie Zhang, Zhifang Zhang
In this paper, a series of poly ammonium shale inhibitors were prepared from diethylamine, epichlorohydrin, and melamine (DEM) and their inhibition to shale were evaluated by bentonite linear expansion test, anti-swelling experiments, and mud ball experiments. Additionally, other properties of drilling fluid treated by poly ammonium were evaluated. Anti-swelling results showed that anti-swelling rate of DEM-8 reaches up to 97.8% when its concentration reaches to 0.8%. Mud ball experiment and drilling fluid evaluation showed DEM-8 has strong inhibitive capability to bentonite hydration swelling and controlling the particle size of bentonite in a large scale...
April 25, 2018: Chemistry Central Journal
Min Wei, Wenyang Zhang
In this work, a novel aptamer-based electrochemical biosensor was developed for the determination of Ochratoxin A (OTA) by using carbon aerogels (CAs) and methylene blue (MB) as signal amplification strategy. CAs was used as carrier to load the abundant of complementary DNA (cDNA), which could enhance the hybridization between CAs-cDNA and aptamer immobilized on the electrode surface, thus provide more double-stranded DNA for MB intercalation. The current of MB on the CAs-cDNA/apt/AuE sensor was twice that on the cDNA/apt/AuE sensor, which indicated that the CAs with high surface area enabled a higher loading of the cDNA and absorbed more MB, thus realized the signal amplification strategy...
April 25, 2018: Chemistry Central Journal
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