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Chemistry Central Journal

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https://read.qxmd.com/read/30570683/microwave-synthesis-crystal-structure-antioxidant-and-antimicrobial-study-of-new-6-heptyl-5-6-dihydrobenzo-4-5-imidazo-1-2-c-quinazoline-compound
#1
Hiba Ali Hasan, Emilia Abdulmalek, Mohd Basyaruddin Abdul Rahman, Khozirah Binti Shaari, Bohari Mohd Yamin, Kim Wei Chan
BACKGROUND: Although the development of antibiotic and antioxidant manufacturing, the problem of bacterial resistance and food and/or cosmetics oxidation still needs more efforts to design new derivatives which can help to minimize these troubles. Benzimidazo[1,2-c]quinazolines are nitrogen-rich heterocyclic compounds that possess many pharmaceutical properties such as antimicrobial, anticonvulsant, immunoenhancer, and anticancer. RESULTS: A comparative study between two methods, (microwave-assisted and conventional heating approaches), was performed to synthesise a new quinazoline derivative from 2-(2-aminophenyl)-1H-benzimidazole and octanal to produce 6-heptyl-5,6-dihydrobenzo[4,5]imidazo[1,2-c]quinazoline (OCT)...
December 20, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30570680/determination-of-antioxidant-and-antimicrobial-activities-of-the-extracts-of-aerial-parts-of-portulaca-quadrifida
#2
Zelalem Yibralign Desta, Desie Alemaw Cherie
BACKGROUND: The extracts from the aerial parts of Portulaca quadrifida have been reported to show the total flavonoid content, antioxidant and antibacterial activities. RESULTS: Our results revealed that the total flavonoid content of methanol and chloroform extracts is 2.335 ± 0.0097 and 1.7312 ± 0.0082 mgQE/100 g respectively. The two extracts also showed good antioxidant activity and total phenolic content as well as weak to moderate antibacterial activity against some bacteria...
December 20, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569337/analysis-of-coumarin-and-angelica-lactones-in-smokeless-tobacco-products
#3
Kevin McAdam, Trevor Enos, Carol Goss, Harriet Kimpton, Arif Faizi, Steve Edwards, Christopher Wright, Andrew Porter, Brad Rodu
Differences in health risks between different styles of smokeless tobacco products (STPs) have prompted interest in their relative levels of toxic chemicals. We report here the development of methods for the analysis of STPs for coumarin and for α-angelica lactone (α-AL), both of which have been included in various published lists of tobacco toxicants. We have also determined the concentrations of these lactones in commercial STPs from the US and Sweden, representing 80-90% of the 2010 market share for all the major STP categories in these two countries: 65 products (plus two reference products) for coumarin and 66 commercial products for α-AL...
December 20, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569261/development-of-a-practical-synthesis-of-etravirine-via-a-microwave-promoted-amination
#4
Da Feng, Fenju Wei, Zhao Wang, Dongwei Kang, Peng Zhan, Xinyong Liu
BACKGROUND: Etravirine (ETV) was approved as the second generation drug for use in individuals infected with HIV-1 in 2008 by the U.S. FDA with its unique antiviral activity, high specificity, and low toxicity. However, there are some shortcomings of the existing synthetic routes, such as the long reaction time and poor yield. RESULTS: This article describes our efforts to develop an efficient, practical, microwave-promoted synthetic method for one key intermediate of ETV, which is capable of being operated on a scale-up synthesis level...
December 20, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569247/ligand-exchange-method-for-determination-of-mole-ratios-of-relatively-weak-metal-complexes-a-comparative-study
#5
Mokhtar Mabrouk, Sherin F Hammad, Mohamed A Abdelaziz, Fotouh R Mansour
Ligand exchange method is introduced as an alternative to Job's and mole ratio methods for studying the stoichiometry of relatively weak metal complexes in solutions. The method involves adding varying amounts of a ligand (L) to an excess constant amount of a colored complex (MX) with appropriate stability and molar absorptivity. The absorbance of each solution is measured at the λmax of the initial complex, MX, and plotted against the concentration of the studied ligand, L. If the newly formed complex ML does not absorb at the λmax of the initial complex, then attenuation of the absorbance of the initial complex on adding varying quantities of the investigational ligand gives an inverse calibration line that intersects with the calibration curve of initial complex at a given point...
December 20, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569392/design-synthesis-and-therapeutic-potential-of-3-2-1h-benzo-d-imidazol-2-ylthio-acetamido-n-substituted-phenyl-benzamide-analogues
#6
Sumit Tahlan, Kalavathy Ramasamy, Siong Meng Lim, Syed Adnan Ali Shah, Vasudevan Mani, Balasubramanian Narasimhan
BACKGROUND: The emergence of bacterial resistance is a major public health problem. It is essential to develop and synthesize new therapeutic agents with better activity. The mode of actions of certain newly developed antimicrobial agents, however, exhibited very limited effect in treating life threatening systemic infections. Therefore, the advancement of multi-potent and efficient antimicrobial agents is crucial to overcome the increased multi-drug resistance of bacteria and fungi. Cancer, which remains as one of the primary causes of deaths and is commonly treated by chemotherapeutic agents, is also in need of novel and efficacious agents to treat resistant cases...
December 19, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569323/novel-glitazones-as-ppar%C3%AE-agonists-molecular-design-synthesis-glucose-uptake-activity-and-3d-qsar-studies
#7
Subhankar P Mandal, Aakriti Garg, P Prabitha, Ashish D Wadhwani, Laxmi Adhikary, B R Prashantha Kumar
BACKGROUND: An alarming requirement for finding newer antidiabetic glitazones as agonists to PPARγ are on its utmost need from past few years as the side effects associated with the available drug therapy is dreadful. In this context, herein, we have made an attempt to develop some novel glitazones as PPARγ agonists, by rational and computer aided drug design approach by implementing the principles of bioisosterism. The designed glitazones are scored for similarity with the developed 3D pharmacophore model and subjected for docking studies against PPARγ proteins...
December 19, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569203/synthesis-biological-evaluation-and-molecular-docking-studies-of-6-4-nitrophenoxy-1h-imidazo-4-5-b-pyridine-derivatives-as-novel-antitubercular-agents-future-dpre1-inhibitors
#8
Jineetkumar Gawad, Chandrakant Bonde
Tuberculosis is an air-borne disease, mostly affecting young adults in their productive years. Here, Ligand-based drug design approach yielded a series of 23 novel 6-(4-nitrophenoxy)-1H-imidazo[4,5-b]pyridine derivatives. The required building block of imidazopyridine was synthesized from commercially available 5,5-diaminopyridine-3-ol followed by four step sequence. Derivatives were prepared using various substituted aromatic aldehydes. All the synthesized analogues were characterized using NMR, Mass analysis and also screened for in vitro antitubercular activity against Mycobacterium tuberculosis (H37 Rv)...
December 19, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30569201/classification-of-different-pineapple-varieties-grown-in-malaysia-based-on-volatile-fingerprinting-and-sensory-analysis
#9
Ola Lasekan, Fatma Khalifa Hussein
BACKGROUND: Pineapple is highly relished for its attractive sweet flavour and it is widely consumed in both fresh and canned forms. Pineapple flavour is a blend of a number of volatile and non-volatile compounds that are present in small amounts and in complex mixtures. The aroma compounds composition may be used for purposes of quality control as well as for authentication and classification of pineapple varieties. RESULTS: The key volatile compounds and aroma profile of six pineapple varieties grown in Malaysia were investigated by gas chromatography-olfactometry (GC-O), gas-chromatography-mass spectrometry and qualitative descriptive sensory analysis...
December 19, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30564984/therapeutic-importance-of-synthetic-thiophene
#10
REVIEW
Rashmi Shah, Prabhakar Kumar Verma
Thiophene and its substituted derivatives are very important class of heterocyclic compounds which shows interesting applications in the field of medicinal chemistry. It has made an indispensable anchor for medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules. It has been reported to possess a wide range of therapeutic properties with diverse applications in medicinal chemistry and material science, attracting great interest in industry as well as academia...
December 19, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30564982/palladium-catalyzed-borylation-of-aryl-pseudo-halides-and-its-applications-in-biaryl-synthesis
#11
Hong Ji, Jianghong Cai, Nana Gan, Zhaohua Wang, Liyang Wu, Guorong Li, Tao Yi
A facile and efficient palladium-catalyzed borylation of aryl (pseudo)halides at room temperature has been developed. Arylboronic esters were expeditiously assembled in good yields and with a broad substrate scope and good functional group compatibility. This approach has been successfully applied to the one-pot two-step borylation/Suzuki-Miyaura cross-coupling reaction, providing a concise access to biaryl compounds from readily available aryl halides. Furthermore, a parallel synthesis of biaryl analogs is accomplished at room temperature using the strategy, which enhances the practical usefulness of this method...
December 19, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30556121/chemical-composition-antioxidant-and-antimicrobial-potential-of-essential-oils-from-different-parts-of-daphne-mucronata-royle
#12
Iqra Ashraf, Muhammad Zubair, Komal Rizwan, Nasir Rasool, Muhammad Jamil, Shakeel Ahmad Khan, Rasool Bakhsh Tareen, Viqar Uddin Ahmad, Abid Mahmood, Muhammad Riaz, M Zia-Ul-Haq, Hawa Ze Jaafar
This research work was executed to determine chemical composition, anti-oxidant and anti-microbial potential of the essential oils extracted from the leaves and stem of Daphne mucronata Royle. From leaves and stem oils fifty-one different constituents were identified through GC/MS examination. The antioxidant potential evaluated through DPPH free radical scavenging activity and %-inhibition of peroxidation in linoleic acid system. The stem's essential oil showed the good antioxidant activity as compared to leaves essential oil...
December 17, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30523481/preparation-optimization-and-swelling-study-of-carboxymethyl-sago-starch-cmss-acid-hydrogel
#13
Nur Fattima' Al-Zahara' Tuan Mohamood, Norhazlin Zainuddin, Mansor Ahmad Ayob, Sheau Wei Tan
In this study, sago starch was modified in order to enhance its physicochemical properties. Carboxymethylation was used to introduce a carboxymethyl group into a starch compound. The carboxymethyl sago starch (CMSS) was used to prepare smart hydrogel by adding acetic acid into the CMSS powder as the crosslinking agent. The degree of substitution of the CMSS obtained was 0.6410. The optimization was based on the gel content and degree of swelling of the hydrogel. In this research, four parameters were studied in order to optimize the formation of CMSS-acid hydrogel...
December 6, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30523436/synthesis-characterization-molecular-docking-analgesic-antiplatelet-and-anticoagulant-effects-of-dibenzylidene-ketone-derivatives
#14
Tauqeer Ahmed, Arif-Ullah Khan, Muzaffar Abbass, Edson Rodrigues Filho, Zia Ud Din, Aslam Khan
In this study dibenzylidene ketone derivatives (2E,5E)-2-(4-methoxybenzylidene)-5-(4-nitrobenzylidene) cyclopentanone (AK-1a) and (1E,4E)-4-(4-nitrobenzylidene)-1-(4-nitrophenyl) oct-1-en-3-one (AK-2a) were newly synthesized, inspired from curcuminoids natural origin. Novel scheme was used for synthesis of AK-1a and AK-2a. The synthesized compounds were characterized by spectroscopic techniques. AK-1a and AK-2a showed high computational affinities (E-value > - 9.0 kcal/mol) against cyclooxygenase-1, cyclooxygenase-2, proteinase-activated receptor 1 and vitamin K epoxide reductase...
December 6, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30519833/sodium-dichloroisocyanurate-delays-ripening-and-senescence-of-banana-fruit-during-storage
#15
Qixian Wu, Taotao Li, Xi Chen, Lingrong Wen, Ze Yun, Yueming Jiang
Banana as a typical climacteric fruit soften rapidly, resulting in a very short shelf life after harvest. Sodium dichloroisocyanurate (NaDCC) is reported to be an effectively antibacterial compound. Here, we investigated the effects of NaDCC on ripening and senescence of harvested banana fruit at physiological and molecular levels. Application of 200 mg L-1 NaDCC solution effectively inhibited the ripening and senescence of banana fruit after harvest. NaDCC treatment reduced greatly ethylene production rate and expressions of genes encoding 1-aminocyclopropane-1-carboxylate synthetase, 1-aminocyclopropane-1-carboxylate oxidase, ethylene-responsive transcription factor and EIN3-binding F-box protein...
December 5, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30519801/a-modified-method-of-separating-tl-i-and-tl-iii-in-aqueous-samples-using-solid-phase-extraction
#16
Qingxiang Xiao, Atta Rasool, Tangfu Xiao, Philippe C Baveye
In spite of the development of new measurement techniques in recent years, the rapid and accurate speciation of thallium in environmental aqueous samples remains a challenge. In this context, a novel method of solid phase extraction (SPE), involving the anion exchange resin AG1-X8, is proposed to separate Tl(I) and Tl(III). In the presence of diethylene triamine pentacetate acid (DTPA), Tl(III) and Tl(I) can be separated by selective adsorption of Tl(III)-DTPA onto the resin, Tl(III) is then eluted by a solution of HCl with SO2 ...
December 5, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30515643/design-synthesis-and-biological-evaluation-of-3-2-aminooxazol-5-yl-2h-chromen-2-one-derivatives
#17
Saloni Kakkar, Sanjiv Kumar, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah, Balasubramanian Narasimhan
BACKGROUND: In view of wide range of biological activities of oxazole, a new series of oxazole analogues was synthesized and its chemical structures were confirmed by spectral data (Proton/Carbon-NMR, IR, MS etc.). The synthesized oxazole derivatives were screened for their antimicrobial and antiproliferative activities. RESULTS AND DISCUSSION: The antimicrobial activity was performed against selected fungal and bacterial strains using tube dilution method. The antiproliferative potential was evaluated against human colorectal carcinoma (HCT116) and oestrogen- positive human breast carcinoma (MCF7) cancer cell lines using Sulforhodamine B assay and, results were compared to standard drugs, 5-fluorouracil and tamoxifen, respectively...
December 4, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30515636/molecular-docking-studies-of-coumarin-hybrids-as-potential-acetylcholinesterase-butyrylcholinesterase-monoamine-oxidase-a-b-and-%C3%AE-amyloid-inhibitors-for-alzheimer-s-disease
#18
REVIEW
Samina Khan Yusufzai, Mohammad Shaheen Khan, Othman Sulaiman, Hasnah Osman, Dalily Nabilah Lamjin
Coumarins are the phytochemicals, which belong to the family of benzopyrone, that display interesting pharmacological properties. Several natural, synthetic and semisynthetic coumarin derivatives have been discovered in decades for their applicability as lead structures as drugs. Coumarin based conjugates have been described as potential AChE, BuChE, MAO and β-amyloid inhibitors. Therefore, the objective of this review is to focus on the construction of these pharmacologically important coumarin analogues with anti-Alzheimer's activities, highlight their docking studies and structure-activity relationships based on their substitution pattern with respect to the selected positions on the chromen ring by emphasising on the research reports conducted in between year 1968 to 2017...
December 4, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30515635/synthesis-sar-and-in-vitro-therapeutic-potentials-of-thiazolidine-2-4-diones
#19
Sucheta, Sumit Tahlan, Prabhakar Kumar Verma
BACKGROUND: Thiazolidinedione is a pentacyclic moiety having five membered unsaturated ring system composed with carbon, oxygen, nitrogen and sulfur molecules at 1 and 3 position of the thiazole ring and widely found throughout nature in various form. They favourably alter concentration of the hormones secreted by adipocytes, particularly adiponectin. They also increase total body fat and have mixed effects on circulating lipids. Thiazolidinedione nucleus is present in numerous biological moieties and has different pharmacological activities likes, e...
December 4, 2018: Chemistry Central Journal
https://read.qxmd.com/read/30511321/temperature-dependent-control-of-the-solubility-of-gallium-nitride-in-supercritical-ammonia-using-mixed-mineralizer
#20
Daisuke Tomida, Kiyoshi Kuroda, Kentaro Nakamura, Kun Qiao, Chiaki Yokoyama
Using a mass-loss method, we investigated the solubility change of gallium nitride (GaN) in supercritical ammonia with mixed mineralizers [ammonium chloride (NH4 Cl) + ammonium bromide (NH4 Br) and NH4 Cl + ammonium iodide (NH4 I)]. The solubilities were measured over the temperature range 450-550 °C, at 100 MPa. The solubility increased with NH4 Cl mole fraction at 450 °C and 100 MPa. The temperature dependence of the solubility curve was then measured at an equal mole ratio of the two mineralizers...
December 3, 2018: Chemistry Central Journal
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