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Chemistry Central Journal

Komal Rizwan, Nasir Rasool, Ravya Rehman, Tariq Mahmood, Khurshid Ayub, Tahir Rasheed, Gulraiz Ahmad, Ayesha Malik, Shakeel Ahmad Khan, Muhammad Nadeem Akhtar, Noorjahan Banu Alitheen, Muhammad Nazirul Mubin Aziz
A variety of imine derivatives have been synthesized via Suzuki cross coupling of N-(4-bromophenyl)-1-(3-bromothiophen-2-yl)methanimine with various arylboronic acids in moderate to good yields (58-72%). A wide range of electron donating and withdrawing functional groups were well tolerated in reaction conditions. To explore the structural properties, Density functional theory (DFT) investigations on all synthesized molecules (3a-3i) were performed. Conceptual DFT reactivity descriptors and molecular electrostatic potential analyses were performed by using B3LYP/6-31G(d,p) method to explore the reactivity and reacting sites of all derivatives (3a-3i)...
July 17, 2018: Chemistry Central Journal
Xiaobin Wang, Zhengjiao Ren, Mengqi Wang, Min Chen, Aiming Lu, Weijie Si, Chunlong Yang
BACKGROUND: Tetramic acid, thiophene and hydrazone derivatives were found to exhibit favorable antifungal activity. Aiming to discover novel template molecules with potent antifungal activity, a series of novel 3-(thiophen-2-yl)-1,5-dihydro-2H-pyrrol-2-one derivatives containing a hydrazone group were designed, synthesized, and evaluated for their antifungal activity. RESULTS: The structures of 3-(thiophen-2-yl)-1,5-dihydro-2H-pyrrol-2-one derivatives bearing a hydrazone group were confirmed by FT-IR, 1 H NMR, 13 C NMR, 1 H-1 H NOESY, EI-MS and elemental analysis...
July 17, 2018: Chemistry Central Journal
Ke Li, Fan Yao, Qiang Xue, Hang Fan, Lingguang Yang, Xiang Li, Liwei Sun, Yujun Liu
A flavonoids-rich extract of Scutellaria baicalensis shoots and its eight high content flavonoids were investigated for their inhibitory effects against α-glucosidase and α-amylase. Results show that abilities of the extract in inhibiting the two enzymes were obviously higher than those of acarbose. Moreover, inhibitory abilities of all the eight individual flavonoids against the two enzymes show exactly a same order (i.e., apigenin > baicalein > scutellarin > chrysin > apigenin-7-O-glucuronide > baicalin > chrysin-7-O-glucuronide > isocarthamidin-7-O-glucuronide), and their structure-activity relationship could be well-interpretated by the refined assign-score method...
July 12, 2018: Chemistry Central Journal
Emmanuel O Oyelude, Johannes A M Awudza, Sylvester K Twumasi
The removal of malachite green (MG) from aqueous solution using teak leaf litter powder (TLLP) was investigated. The process was influenced by initial concentration, pH and temperature of dye solution as well as TLLP dosage. Optimum removal of MG per gram of TLLP occurred at 2 g/L and at pH 6-8. Dubinin-Radushkevich and Freundlich isotherm models fit the batch adsorption data better than Langmuir isotherm. The monolayer capacity of TLLP was 333.33 mg/g at 293-313 K. The mean free energy of 7.07 kJ/mol implied physical adsorption...
July 11, 2018: Chemistry Central Journal
Yousef Alqaheem, Abdulaziz Alomair, Abdulwahab Alhendi, Sharifah Alkandari, Nusrat Tanoli, Nourah Alnajdi, Andrés Quesada-Peréz
Polymeric membranes are usually prepared from solvents like n-methylpyrrolidone (NMP) because of the strong dissolving power and high boiling point. Yet, the solvent is costly, toxic and has environmental issues. In this work, nontoxic solvents such as methyl L-lactate, ethyl lactate, propylene carbonate, tributyl o-acetylcitrate, tributyl citrate, triethyl phosphate, and γ-butyrolactone (GBL) were introduced during membrane preparation. It was found that all the solvents were unable to dissolve polyetherimide except GBL...
July 10, 2018: Chemistry Central Journal
Yi-Jun Liao, Xiao-Li Wu, Lin Zhu, Tao Yi
BACKGROUND: Although polypropylene (PP) has been widely used, its brittleness restricts even further applications. METHODS: In this study, we have used a melt blending process to synthesize styrene acrylonitrile (SAN)/PP blends containing 0, 5, 10, 15 and 20 wt% SAN. The effects of adding various amount of SAN on the blends characteristics, mechanical properties, thermal behavior and morphology were investigated. RESULTS: The results demonstrated that SAN had no obviously effect on crystal form but reduced the crystallinity of PP and increased the viscosity...
July 9, 2018: Chemistry Central Journal
Mashallah Rezakazemi, Mohsen Maghami, Toraj Mohammadi
Phenolic wastewater was treated using anaerobic submerged membrane bioreactor (ASMBR). Effect of different solids retention times on MBR performance was studied. Various ratios of carbon to nitrogen were used in the synthetic wastewaters. During the operation, phenol concentration of feed was changed from 100 to 1000 mg L-1 . Phenol concentration was increased stepwise over the first 30 days and kept constant at 1000 mg L-1 , thereafter. For the first 100 days, a chemical oxygen demand (COD) to N ratio of 100:5...
July 9, 2018: Chemistry Central Journal
Mohammad Reza Rezaei Kahkha, Ali Reza Oveisi, Massoud Kaykhaii, Batool Rezaei Kahkha
A stable and porous amino-functionalized zirconium-based metal organic framework (Zr-MOF-NH2 ) containing missing linker defects was prepared and fully characterized by FTIR, scanning electron microscopy, powder X-ray diffraction, and BET surface area measurement. The Zr-MOF-NH2 was then applied as an adsorbent in pipette-tip solid phase extraction (PT-SPE) of carbamazepine. Important parameters affecting extraction efficiency such as pH, sample volume, type and volume of eluent, amount of adsorbent, and number of aspirating/dispensing cycles for sample solution and eluent solvent were investigated and optimized...
June 30, 2018: Chemistry Central Journal
Anderson Wilbur Lopes Andrade, Keylla da Conceição Machado, Katia da Conceição Machado, Daiana Dias Ribeiro Figueiredo, Jorge Mauricio David, Muhammad Torequl Islam, Shaikh Jamal Uddin, Jamil A Shilpi, Jéssica Pereira Costa
PURPOSE: Free radicals are considered as the causative agents of a variety of acute and chronic pathologies. Natural antioxidants have drawn attention of the researchers in recent years for their ability to scavenge free radicals with minimal or even no side effects. This study evaluates the antioxidant capacity of agathisflavone, a naturally occurring biflavonoid by a number of in vitro methods. METHODS: Agathisflavone was subjected to DPPH, ABTS, OH and NO radical scavenging assay, reducing potential and inhibition of lipid peroxidation (TBARS) test using trolox as a standard...
June 29, 2018: Chemistry Central Journal
Guofan Jin, Fuyan Xiao, Ruijiang Liu
(Z,Z')-1,1'-(4-ortho-Caboranyldimethyl)-bis(2-methoxyphenylethan-1-oxime) intermediate 3 was synthesized by a three-step reaction with a final treatment with base to give a new series of ortho-carboranyl biphenyloxime derivatives (4-8). Compounds 7 and 8 showed high solubility and the in vitro study results revealed high levels of accumulation in HeLa cells with higher cytotoxicity and boron uptake compared to L-boronphenylalanine.
June 29, 2018: Chemistry Central Journal
Sanjiv Kumar, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah, Balasubramanian Narasimhan
BACKGROUND: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies. RESULTS: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means...
June 25, 2018: Chemistry Central Journal
Erik Andrade-Jorge, José Bribiesca-Carlos, Francisco J Martínez-Martínez, Marvin A Soriano-Ursúa, Itzia I Padilla-Martínez, José G Trujillo-Ferrara
Dioxoisoindolines have been included as a pharmacophore group in diverse drug-like molecules with a wide range of biological activity. Various reports have shown that phthalimide derivatives are potent inhibitors of AChE, a key enzyme involved in the deterioration of the cholinergic system during the development of Alzheimer's disease. In the present study, 2-(2-(3,4-dimethoxyphenyl)ethyl)isoindoline-1,3-dione was synthesized, crystallized and evaluated as an AChE inhibitor. The geometric structure of the crystal and the theoretical compound (from molecular modeling) were analyzed and compared, finding a close correlation...
June 25, 2018: Chemistry Central Journal
Jineetkumar Gawad, Chandrakant Bonde
Tuberculosis has proved harmful to the entire history of mankind from past several decades. Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1) is a recent target which was identified in 2009 but unfortunately it is neither explored nor crossed phase II. In past several decades few targets were identified for effective antitubercular drug discovery. Resistance is the major problem for effective antitubercular drug discovery. Arabinose is constituent of mycobacterium cell wall. Biosynthesis of arabinose is FAD dependant two step epimerisation reaction which is catalysed by DprE1 and DprE2 flavoprotein enzymes...
June 23, 2018: Chemistry Central Journal
Wenwen Zhou, Zhitao Liang, Ping Li, Zhongzhen Zhao, Jun Chen
BACKGROUND: Cinnamomi Cortex, the dried stem bark of Cinnamomum cassia Presl (Rougui in Chinese) has been widely used in traditional Chinese medicine, cooking and perfumery for thousands of years. Traditionally, the Cinnamomi Cortex of thick size is considered to be of good quality; however, there is no scientific data to support this point. Considering that essential oils are the main bioactive components, Cinnamomi Cortex of greater variety and amount essential oils is thought to be of better quality...
June 21, 2018: Chemistry Central Journal
Yasser H Zaki, Marwa S Al-Gendey, Abdou O Abdelhamid
BACKGROUND: Chalcones have a place with the flavonoid family and show a few very important pharmacological activities. They can used as initial compounds for synthesis of several heterocyclic compounds. The compounds with the backbone of chalcones have been reported to possess various biological activities. RESULTS: Pyridine and thioamide derivatives were obtained from the reaction of 3-(furan-2-yl)-1-(p-tolyl)prop-2-en-1-one with the appropriate amount of malononitrile, benzoylacetonitrile, ethyl cyanoacetate and thiosemicarbazide in the presence of ammonium acetate...
June 20, 2018: Chemistry Central Journal
Samina Khan Yusufzai, Hasnah Osman, Mohammad Shaheen Khan, Basma M Abd Razik, Mohammed Oday Ezzat, Suriyati Mohamad, Othman Sulaiman, Jualang Azlan Gansau, Thaigarajan Parumasivam
A series of novel 4-thiazolidinone inhibitors SKYa-SKYg, containing coumarin as a core structure were synthesized via facile and efficient method. The structures of the synthesized compounds were established by extensive spectroscopic studies (FT IR, 1D NMR, 2D NMR, LC-MS) and elemental analysis. All the synthesized hybrids were further evaluated for their potential as anti-tubercular agents against Mycobacterium tuberculosis H37Rv ATCC 25618, and anti-bacterial agents against Escherichia coli, Enterobacter aerogenes, Salmonella typhi, Streptococcus pneumoniae and Staphylococcus aureus...
June 12, 2018: Chemistry Central Journal
Wesam S Shehab, Magda H Abdellattif, Samar M Mouneir
BACKGROUND: Chalcones are intent in the daily diet as a favorable chemotherapeutic compound; on the other hand thiophene moiety is present in a large number of bioactive molecules having diverse biological efficiency. RESULTS: Our current goal is the synthesis of (E)-1-(pyridin-3-yl)-3-(thiophen-2-yl) prop-2-en-1-one 3 that' s used as a starting compound to synthesize the novel pyrimidine-2-thiol, pyrazole, pyran derivatives. Chalcones 3 was prepared by condensation of 3-acetylpyridine with thiophene 2-carboxaldehyde which reacted with thiourea to obtain pyrimidinthiol derivative 4...
June 8, 2018: Chemistry Central Journal
Souha H Youssef, Maha Abdel-Monem Hegazy, Dalia Mohamed, Amr Mohamed Badawey
Paracetamol (PAR), Pseudoephedrine hydrochloride (PSE) and cetirizine dihydrochloride (CET) is a ternary mixture that composes tablets which are popular for the relief of flu in Egypt. The spectra of the drugs were overlapped and no spectrophotometric methods were reported to resolve the mixture. This research proposes four spectrophotometric methods that are efficient and require water only as a solvent. The first method was ratio subtraction-ratio difference method (RSDM) where PAR was initially removed from the mixture by ratio subtraction and determined at 292...
June 1, 2018: Chemistry Central Journal
Snehlata Yadav, Siong Meng Lim, Kalavathy Ramasamy, Mani Vasudevan, Syed Adnan Ali Shah, Abhishek Mathur, Balasubramanian Narasimhan
BACKGROUND: The study describes the synthesis, characterization, in vitro antimicrobial and anticancer evaluation of a series of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamide derivatives. The synthesized derivatives were also assessed for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The compounds found active in in vitro study were assessed for their in vivo antitubercular activity in mice models and for their inhibitory action on vital mycobacterial enzymes viz, isocitrate lyase, pantothenate synthetase and chorismate mutase...
May 26, 2018: Chemistry Central Journal
Niyaz Ahmad, Rizwan Ahmad, Md Aftab Alam, Farhan Jalees Ahmad
BACKGROUND: Doxorubicin hydrochloride (DOX·HCl), an anthracycline glycoside antibiotic, exhibits low oral bioavailability due to active efflux from intestinal P-glycoprotein receptors. The oral administration of DOX remains a challenge hence; no oral formulation for DOX is marketed, till date. AIM OF THE STUDY: To improve the oral bioavailability of DOX through, preparation of a nanoformulation i.e. PEGylated-doxorubicin(DOX)-loaded-poly-lactic-co-glycolic acid (PLGA)-Nanoparticles (NPs) and to develop and validate an ultra-high performance liquid chromatography electrospray ionization-synapt mass spectrometric bioanalytical method (UHPLC/ESI-QTOF-MS/MS) for plasma (Wistar rats) DOX quantification...
May 23, 2018: Chemistry Central Journal
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