Catalyst-Free Expeditious Synthesis Of 2-(4-TERT-BUTYLPHENYL)-3-Sustituted Quinazolin-4(3H)-One Derivatives

Quinazoline and quinazolinone derivatives are well-known bioactive heterocycles owing to their therapeutic diversity and extensive medicinal application in drug design and pharmaceutics. A series of 2-(4-tert-butylphenyl)-3-substituted quinazolin-4(3H)-one derivatives, 2a-q was herein synthesized from benzoylational conversion of anthranilic acid to 2-(4-tertbutylphenyl)-4H-3,1-benzoxazin-4-one, 1 which was the first precursor which was subsequently transformed to the targeted 2,3-disubstituted quinazolin-4(3H)-one derivatives, 2a-q by reacting with some cheap and readily accessible amino-containing moieties via an ameliorable pathway. The catalyst-free synthesis was successfully achieved by careful reaction optimization study using solvent choice and reaction temperature variability as key parameters. The chemical structures of the synthesized compounds were confirmed by IR, UV, 1H-NMR, 13C-NMR and DEPT-135 as well as analytical data. The data obtained were consistent with the proposed structures of the compounds. This targeted quinazoline motifs might pave way for new bioactive template from future drug development

Comparison of the antioxidant activity and total phenolic contents in some Stachys species

The methanolic extracts of the aerial parts of nine Stachys species: S. persica Gmel., S. fruticulosa M. B., S. laxa Boiss. & Buhse., S. inflata Benth., S. turcomanica Trautv., S. subaphylla Rech. F., S. setiferaC. A. Mey., S. byzantina C. Koch and S. trinervis Aitch. & Hemsl. were investigated for their antioxidant activity and total phenolic content using FRAP and Folin-Ciocalteu assays respectively. S. persica Gmel. and S. fruticulosa M. B. had the highest antioxidant activity (61.42 and 62.02 mmol FeII/100g) and total phenolic content (3294.96 and 4450.36 mg gallic acid/100 g) among these nine species. There was a direct correlation between total phenol and antioxidant activity (R2 = 0.9446, p 0.001) which indicates that polyphenols are the main antioxidants

Characterization, Proximate Composition and Evaluation of Antimicrobial Activity of Seed Oil of Bauhinia tomentosa

Background: This study was carried out to investigate proximate composition, phytochemical profile and antimicrobial activity of the spectroscopically characterized seed oil of Bauhinia tomentosa . Materials and method: The characterization was carried out using FT-IR, mass spectra, 1H- and 13C-NMR. Results: The results from the proximate analysis showed the presence of crude protein 30.36±0.98%, crude fibre 26.00±0.69%, carbohydrate 25.32±0.57%, moisture content 12.04±0.39%, ash content 4.00±0.15% and fat content 2.28±0.09%. The phytochemical screening revealed the presence of alkaloids, flavonoids, saponins, terpenes, cardiac glycosides, sterols, anthraquinones and tannins in varying degrees. The mineral determination showed that the seed oil contained iron (3.10±0.01 mg kgG1), manganese (0.38±0.01 mg kgG1), while cadmium (0.0 mg kgG1), lead (0.0 mg kgG1) and nickel (0.0 mg kgG1) were not detected. The extracted seed oil was investigated for antimicrobial efficiency against four bacterial isolates and two fungal, wherein gentamicin and clotrimazole were the clinical standard antibiotic and antifungal agents, respectively. Conclusion: The antimicrobial activity result revealed the sample to be bioactive and of great pharmaceutical potential with MIC value of 6.25 and <3.625 mg mLG1 against Escherichia coli and Candida albican, respectively. Due to high nutritional values and broad antimicrobial properties, the seed oil of Bauhinia tomentosa has nutraceutical potentials, which might pave way for its use as an alternative nutrient source for mankind or for industrial purpose

Motivations, Learning and Creativity in Online Citizen Sceince Charlene Jennett, Laure Kloetzer, Daniel Schneider, Ioanna Iacovides, Anna L. Cox, Margaret Gold, Brian Fuchs, Alexandra Eveleigh, Kathleen Mathieu, Zoya Ajani and Yasmin Talsi

Online citizen science projects have demonstrated their usefulness for research, however little is known about the potential benefits for volunteers. We conducted 39 interviews (28 volunteers, 11 researchers) to gain a greater understanding of volunteers' motivations, learning and creativity (MLC). In our MLC model we explain that participating and progressing in a project community provides volunteers with many indirect opportunities for learning and creativity. The more aspects that volunteers are involved in, the more likely they are to sustain their participation in the project. These results have implications for the design and management of online citizen science projects. It is important to provide users with tools to communicate in order to supporting social learning, community building and sharing.This article is licensed under the terms of the Creative Commons Attribution - NonCommercial - NoDerivativeWorks 4.0 License. The article attached is the publisher's pdf

Phase I/II study of S-1 combined with paclitaxel in patients with unresectable and/or recurrent advanced gastric cancer

Both paclitaxel and S-1 are effective against gastric cancer, but the optimal regimen for combined chemotherapy with these drugs remains unclear. This phase I/II study was designed to determine the maximum tolerated dose (MTD), recommended dose (RD), dose-limiting toxicity (DLT), and objective response rate of paclitaxel in combination with S-1. S-1 was administered orally at a fixed dose of 80 mg m−2 day−1 from days 1 to 14 of a 28-day cycle. Paclitaxel was given intravenously on days 1, 8, and 15, starting with a dose of 40 mg m−2 day−1. The dose was increased in a stepwise manner to 70 mg m−2. Treatment was repeated every 4 weeks unless disease progression was confirmed. In the phase I portion, 17 patients were enrolled. The MTD of paclitaxel was estimated to be 70 mg m−2 because 40% of the patients given this dose level (two of five) had DLT. The RD was determined to be 60 mg m−2. In the phase II portion, 24 patients, including five with assessable disease who received the RD in the phase I portion, were evaluated. The median number of treatment courses was six (range: 1–17). The incidence of the worst-grade toxicity in patients given the RD was 28 and 8%, respectively. All toxic effects were manageable. The response rate was 54.1%, and the median survival time was 15.5 months. Our phase I/II trial showed that S-1 combined with paclitaxel is effective and well tolerated in patients with advanced gastric cancer

Long-Term Survival of Resected Advanced Gastric Cancer with Hepatic and Pancreatic Invasion

A 64-year-old man was transferred to our division with a suspicion of gastric cancer. Computed tomography showed widespread irregular thickening of the stomach walls close to the liver and pancreas. Gastrointestinal fiberscopy showed a type 5 tumor in the upper to lower stomach, histologically diagnosed as tubular adenocarcinoma. Gastric cancer with hepatic and pancreatic invasion was diagnosed. Distant metastasis was not proven and complete resection was planned. At laparotomy, the tumor showed general expanding growth and invasion through the lateral segment of the liver and pancreas. Total gastrectomy and combined resection of the distal pancreas, spleen and left segment of the liver were performed. Hepatic and pancreatic invasion and lymph node metastasis were microscopically proven. Pancreatic fistula occurred postoperatively. On postoperative days 40, he was discharged. He received two cycles of adjuvant tegafur/gimeracil/oteracil chemotherapy. He has had no sign of recurrence for 7 years and 8 months

Unresectable gastric cancer with gastric outlet obstruction and distant metastasis responding to intraperitoneal and folfox chemotherapy after palliative laparoscopic gastrojejunostomy: report of a case

<p>Abstract</p> <p>Background</p> <p>Gastric outlet obstruction (GOO) caused by unresectable gastric cancer is a challenging aspect of patient care. There have been no reports involving patients with obstructing gastric cancer and several incurable factors curatively treated by multimodal treatments.</p> <p>Case presentation</p> <p>We report a case of 55-year-old man who was diagnosed with a poorly differentiated adenocarcinoma in the pre-pyloric antrum with GOO by gastroscopy. An abdominal computed tomography (CT) scan revealed thickening of the gastric wall and adjacent fat infiltration, and a large amount of food in the stomach suggesting a passage disturbance, enlarged lymph nodes along the common hepatic and left gastric arteries, and multiple hepatic metastases. The serum carcinoembryonic antigen (CEA) level was 343 ng/ml and the carbohydrate antigen (CA) 19-9 level was within normal limits. The patient underwent a laparoscopic gastrojejunostomy for palliation of the GOO. On the 3^rdand 12^thdays after surgery, he received intraperitoneal chemotherapy with 40 mg of docetaxel and 150 mg of carboplatin. Simultaneously, combined chemotherapy with 85 mg/m²of oxaliplatin for the 1^stday and 600 mg/m²of 5-FU for 2 days (FOLFOX regimen) was administered from the 8^thpost-operative day. After completion of nine courses of FOLFOX, the patient achieved a complete response (CR) with complete disappearance of the primary tumor and the metastatic foci. He underwent a radical subtotal gastrectomy with D3 lymph node dissection 4 months after the initial palliative surgery. The pathologic results revealed no residual primary tumor and no lymph node metastasis in 43 dissected lymph nodes. He has maintained a CR for 18 months since the last operation.</p> <p>Conclusion</p> <p>Combination chemotherapy with systemic and intraperitoneal chemotherapy following laparoscopic bypass surgery showed marked efficacy in the treatment for unresectable advanced gastric cancer with GOO.</p

Adsorption isotherm and kinetics for the removal of nitrate from wastewater using chicken feather fiber

Nitrate has been identified as a major source of water pollution and eutrophication. The use of modified chicken feathers (MCFs) as an adsorbent has not been fully explored. The study therefore assessed the use of MCFs for the adsorption of nitrate. Fresh chicken feathers, obtained from a commercial poultry farm, were first hydrolyzed with sodium hydroxide and activated with HCl ðaqÞ to give modified chicken feathers, MCFs. Experimental constraints were varied in a series of batch tests including concentration, pH, adsorbent dosage and contact time. FTIR was used to monitor the adsorption processes (before and after) of the polluted water. The outcome showed increase in specific surface area and the favorable formation of adsorption sites of MCFs. For the understanding of adsorp�tion mechanism, experimental data were assessed by Langmuir, Freundlich, Temkin and Sips isotherm equations. Pseudo-first and pseudo-second order models were used to evaluate time characteristics of adsorption. The optimum parameters for adsorption are found to be initial ion concentration, initial pH, adsorbent dosage and contact time 300 mg/L, 8, 10 and 480 min, respectively. This study also reveals adsorption fit the chosen isotherm models in the following order: (Sips >Langmuir > Freundlich > Temkin). Sips isotherm having the best fit infers adsorption took place on heterogeneous surface. Pseudo-second-order is suited for explaining nitrate removal based on statistical R2 coefficient. The use of MCFs as an eco-friendly