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Aims Flavonoids and related compounds, such as quercetin‐based antiviral drug Gene‐Eden‐VIR/Novirin, inhibit the protease of severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2). The alkylated chalcones isolated from Angelica keiskei inhibit SARS‐CoV proteases. In this study, we aimed to compare the anti‐SARS CoV‐2 activities of both newly synthesized chalcone derivatives and these two drugs. Methods Determination of the potent antiviral activity of newly synthesized chalcone derivatives against SARS‐CoV‐2 by calculating the RT‐PCR cycling threshold (Ct ) values. Results Antiviral activities of the compounds varied because of being dose dependent. Compound 6, 7, 9, and 16 were highly effective against SARS‐CoV‐2 at the concentration of 1.60 µg/mL. Structure‐based virtual screening was carried out against the most important druggable SARS‐CoV‐2 targets, viral RNA‐dependent RNA polymerase, to identify putative inhibitors that could facilitate the development of potential anti‐coronavirus disease‐2019 drug candidates. Conclusions Computational analyses identified eight compounds inhibiting each target, with binding affinity scores ranging from −4.370 to −2.748 kcal/mol along with their toxicological, ADME, and drug‐like properties.

Staff evaluation, which reshapes with changes and transformations in public administration, is one of the basic elements of personnel management. Registration system had been used as to 2011, after that steps have been taken to transition to performance evaluation system. In this regard, the Ministry of Education has been one of the leading institutions. When some of the performance evaluations of teachers were cancelled by judicial decisions, the application process was stopped for a while and a new evaluation model was introduced. This model was based on 360-degree performance evaluation, which included students and parents in the process. However, the regulation faced reactions from the educational community, trade unions and social media. The aim of this research is to facilitate the shift from registration system to performance evaluation system where it is needed. This transformation applied in the Performance evaluation of teachers affects. The document analysis and semi-structured interview method were used in the study. The research was restricted to the province of İzmir and conducted in the Ministry of National Education. The findings of this research are significant in current developments and trade unions. According to the data obtained as a result of the research, teachers mostly shared negative views on teacher performance evaluation. The performance evaluation system did not make a significant difference from the registry system. The performance evaluation system as applied lagged behind the registry system., Personel değerlendirme, personel yönetiminin temel unsurlarından biridir ve kamu yönetimindeki değişim ve dönüşümlerle birlikte yeniden şekillenmektedir. Türkiye’de 2011 yılına kadar sicil sistemi uygulanmış, 2011 yılı itibariyle sicil sisteminden performans değerlendirme sistemine geçiş için adım atılmıştır. Bu konuda Milli Eğitim Bakanlığı (MEB) öncü kurumlardan biri olmuştur. Öğretmenlere yönelik performans değerlendirmelerinin bir kısmı yargı kararları sonucunda iptal edilince uygulama bir süre durdurulmuş ve daha sonra yeni bir değerlendirme modeli ortaya konmuştur. Yeni model 360 derece performans değerlendirme esasına dayalıdır. 360 derece performans değerlendirme sistemi ile değerlendirme sürecine öğrenci ve veliler de dahil edilmiştir. Ancak düzenleme eğitim camiasından, sendikalardan ve sosyal medyadan gelen tepkilerle karşılaşmıştır. Bu doğrultuda araştırmanın amacı, sicil sisteminden performans değerlendirme sistemine geçişe neden ihtiyaç duyulduğu, performans değerlendirme sisteminin sicil sisteminden farklı bir uygulama getirip getirmediği, performans değerlendirmesinin öğretmenleri nasıl etkilediğini incelemektir. Çalışmada belge analizi ve yarı yapılandırılmış görüşme yöntemi kullanılmıştır. Araştırma, İzmir ili ile sınırlandırılmıştır ve Milli Eğitim Bakanlığı özelinde yürütülmüştür. Araştırma güncel gelişmeleri içermesi ve sendikaları kapsaması bakımından önemlidir. Araştırma sonucunda elde edilen verilere göre, öğretmenler çoğunlukla performans değerlendirmesi hakkında olumsuz görüş taşımaktadır. Performans değerlendirme sistemi, sicil sisteminden önemli bir fark yaratmamıştır. Uygulandığı biçimiyle performans değerlendirme sistemi, sicil sisteminin gerisinde kalmıştır.

The aim of this study is to evaluate the historydepartments and history teaching programs based on the 2015 Higher EducationProgram Atlas data. Higher Education Program Atlas includes the number ofstudents in history and shows the data on which areas students are successfuland in which areas they fail. It also shows which universities are preferredand which universities are preferred in the last ranks. In the study, screeningmodel based on document analysis was used. According to the results of thestudy, it is seen that the net rates of students who settled in the historicaldepartments are low and their success towards numerical courses is close tozero. The fact that the students prefer the history departments because of theprovinces where the departments which are located has been effective. While itwas seen that the scores of the students who settled in the faculties ofeducation were more homogeneous, the faculties of education were found to beweak in terms of the number of students. On the other hand, it is concludedthat the history departments have a high number of students and therefore thestudents who have lower scores could enter to the history department., Bu çalışmada 2018 YÖK ATLAS (Yükseköğretim ProgramAtlası) verileri baz alınarak tarih bölümleri ve tarih öğretmenliği programlarıüzerine değerlendirme yapılmıştır. YÖK ATLAS programı tarih bölümlerineyerleşen öğrencilerin yaptıkları net sayısı, üniversiteye giriş sınavında hangiderslerden başarılı olup hangi derslerden başarısızlık gösterdiklerine ilişkinveriler sunmaktadır. Bu veriler hangi üniversitelerin ilk sıralarda tercihedildiği, hangi üniversitelerin son sıralarda tercih edildiğini degöstermektedir. Araştırmada doküman analizi yönetimi kullanılmıştır.Araştırmanın sonuçlarına göre tarih bölümlerine yerleşen öğrencilerin genelanlamda net ortalamalarının düşük olduğu, sayısal derslere yönelikbaşarılarının sıfıra yakın olduğu görülmüştür. Öğrencilerin tarih bölümlerinitercih etmelerinde tarih bölümlerinin bulunduğu il ve bölümlerin örgün öğrenimolup olmama durumu etkili olmuştur. Eğitim fakültesi tarih öğretmenliğiprogramlarının öğrenci sayısı açısından kontejanlarının az olduğuanlaşılmıştır. Tarih bölümlerinin kontenjanlarının çok fazla olması nedeniylebu bölümlere çok düşük net ortalamasına sahip öğrenciler de yerleşebilmektedir.

The total concentrations of arsenic (As), boron (B), cadmium (Cd), copper (Cu), manganese (Mn), lead (Pb), thallium (Tl) and zinc (Zn) in the mine tailings of an abandoned Pb-Zn mining site and an open boron mining site are investigated in this study. In addition, heavy metals' distributions in chemical binding forms and their mobilities with the presence of binding materials and acidic bacteria are examined. The amounts of sulfur and carbonate in the waste and binding materials are also determined according to the static method, in order to define the acid neutralization potential of the wastes. For mobilization studies, mine tailings are mixed with with leonardite and domestic solid waste compost in different ratios (10/0, 9.5/0.5, 9/1; 8/2). Independent from the binding materials, the mobilization effect of sulfur oxidizing Thiobacillus thiooxidans bacteria has been tested and evaluated. Experiments are conducted using a standard leach test EPA 1310B Extraction Procedure, and correlations between the parameters studied were statistically evaluated using the findings of SPSS 24. Although there is no statistically significant reduction in metals' mobilization with the use of leonardite and waste compost, it has been concluded that different binding agents may have different impacts due to the metal type. As a result, it is understood that metals mobility increases in the presence of Thiobacillus thiooxidans in the environment, and that the heavy metal mobility is directly proportional to the exchangeable and acid soluble fraction, followed by the reducible fraction and the amount of metals bound to the organic fractions.

The present study was carried out in the attempt to synthesize a new class of potential anticancer agents comprising eleven compounds (24-34) sharing the 3,5-diarylisoxazole as a core. The chemical structure of the new synthesized compounds was established by IR, 1H NMR, 13C NMR and elemental analysis. Their biological potential towards prostate cancer was evaluated by using cancer PC3 cells and non-tumorigenic PNT1a cells. Interestingly, compound 26 distinguished from others with a quite high selectivity value that is comparable to 5-FU. The binding mode of 26 towards Ribosomal protein S6 kinase beta-1 (S6K1) was investigated at a molecular level of detail by employing docking simulations based on GLIDE standard precision as well as MM-GBSA calculations.

A stereospecific synthesis of (2S)-3-(2,4,5-trifluorophenyl)propane-1,2-diol from D-mannitol has been developed. The reaction of 2,3-O-isopropylidene-D-glyceraldehyde with 2,4,5-trifluorophenylmagnesium bromide gave [(4R)-2,2-dimethyl-1,3-dioxolan-4-yl](2,4,5-trifluorophenyl)methanol in 65% yield as a mixture of diastereoisomers (1 : 1). The Ph3P catalyzed reaction of the latter with C2Cl6 followed by reduction with Pd/C-catalyzed hydrogenation gave (2S)-3-(2,4,5-trifluorophenyl)propane-1,2-diol with >99% ee and 65% yield.

Starting from (S)-serine, a new method was developed for the synthesis of the β-amino acid part of sitagliptin in ten steps and with an overall yield of 30%. The crucial step of the synthesis was the ring opening of N- and O-protected (R)-aziridin-2-methanol with (2,4,5-trifluorophenyl)magnesium bromide to give N- and O-protected (R)-2-amino-3-(2,4,5-trifluorophenyl)propan-1-ol.

Three new polysubstituted isoindole-1,3-diones were prepared from 2-ethyl-5-hydroxy-3a,4,5,7a-tetrahydro-isoindole-1,3-dione. The reaction of 2-ethyl-5-hydroxy-3a,4,5,7a-tetrahydro-isoindole-1,3-dione with m-CPBA gave the corresponding epoxide. The triacetate derivative was obtained via cis-hydroxylation using OsO4, followed by acetylation. An aromatic derivative, a secondary reaction product, was also formed during the acetylation. Finally, a tricyclic derivative from 2-ethyl-5-hydroxy-3a,4,5,7a-tetrahydro-isoindole-1,3-dione was synthesized via dichloroketene addition under microwave irradiation. The exact structures of epoxide and tricyclic derivatives were determined by X-ray diffraction analysis.

Katı atıklar doğrudan ya da dolaylı olarak fiziksel, kimyasal ve biyolojik olarak çevreyi etkilemektedirler. Nüfus artışı, sanayileşme, kentleşme, teknolojik gelişmeler ve tüketim alışkanlıklarının hızla değişmesi katı atık türlerinin de değişmesine neden olmakta ve bertaraf giderek zorlaşmaktadır. Kentsel katı atıkların ise yaklaşık % 55'i organik atıklardan (mutfak atıkları, hal atıkları vb.) oluşmaktadır. Bu organik atıklar yüksek kirlilik yükleri nedeniyle ya kompostlaştırlır ya da depolama sahalarına gönderilir. Düzenli depolama yöntemi, katı atıkların gideriminde yaygın olarak kullanılmaktadır. Ancak; sızıntı suyunun yer altı suyunu kirletmesi, metan gazının düzgün toplanmadığında sera etkisine sebep olması, katı atık stabilizasyonunun uzun zaman alması nedeniyle fazla arazi kullanımı gibi dezavantajları yavaş yavaş bu yöntemin etkinliğini kaybetmesine neden olmaktadır. Son yıllarda deponilere alternatif olarak biyoreaktör depolama alanları gündeme gelmektedir. Biyoreaktör depolama alanları kentsel katı atıkların kontrollü bir şekilde anaerobik arıtımını sağlamaktadır. Bu tez çalışmasında, kentsel katı atıkların organik kısımlarının farklı aşı çamurları kullanılarak anaerobik biyoreaktörlerdeki arıtma performansları değerlendirilmiştir. Aşı çamuru olarak İzmir'deki Pakmaya tesisinden getirilen anaerobik çamur, piyasadan temin edilen ve tarımda kullanılan sıvı mikrobiyal gübre Bio-One? , Denizli'nin Karahayıt beldesinden alınan sediment çamuru ve Denizli Belediyesi Atıksu Arıtma Tesisi'nden alınan aerobik çamur kullanılmıştır. Aşı çamuru ilave edilen biyoreaktörlerin her biri kontrol grubu (aşı ilavesiz) ile birlikte işletilmiştir. Biyoreaktörler mezofilik koşullarda (35-40°C) ve geri devir uygulamasıyla işletilmiştir. Her bir biyoreaktör 90 gün boyunca işletilmiş ve günlük olarak metan gazı ölçümleri yapılmıştır. Çalışma sonunda, kullanılan aşı çamurlarının tamamında belirli seviyelerde arıtma verimi sağlanırken en yüksek arıtma verimini anaerobik aşı çamuru sağlamıştır. Anaerobik aşı çamuru kullanılan biyoreaktörün sızıntı suyunda başlangıç KOİ konsantrasyonuna göre yaklaşık % 95 bir KOİ azalması sağlanmıştır. Buna ilaveten en yüksek metan yüzdesi (% 70) ve en yüksek metan miktarı (38,94 l) yine bu biyoreaktörde tespit edilmiştir. İşletme boyunca biyoreaktörlerden alınan sızıntı suyu numunelerinde mikrobiyal çeşitliliğin değişimi DGGE yöntemi kullanılarak tespit edilmiştir. Anaerobik aşı çamuru ilaveli biyoreaktörde genelde Methanomicrobiales takımına ait türler teşhis edilirken, Karahayıt çamuru ilaveli biyoreaktörde genelde Methanosarcinales takımına ait türler tespit edilmiştir. Bio-One? aşı ilaveli ve kontrol biyoreaktöründe genelde Methanobacteriales takımına ait türler saptanmıştır. The solid wastes affect the environment as psychical, biological and chemical which can be direct or indirect. Population growth, industrialization, urbanization, technological developments and rapid changes in consumption patterns cause changing in solid waste types and disposal of solid waste is becoming increasingly difficult. 55% of the municipal solid waste occurs from the organic wastes. The organic solid wastes are removed composting or landfilling due to high strenght organic characteristics. The sanitary landfilling technique is widely used in treatment of municipal solid waste. But, a lot of disadvantages as contamination of groundwater by leachate, the greenhouse effect, a long stabilization time cause losing its effectiveness.In recent years, bioreactor landfills have been used as an alternative landfill method to minimize hazard effect of the landfill. The bioreactor landfills provide anaerobic treatment of the municipal solid waste in a controlled condition. In this study, the treatment performance of organic fraction of municipal solid waste was evaluated by using different seed sludge in the anaerobic bioreactor. Bio-one?, anaerobic sludge, karahayıt sludge and aerobic sludge was used as seed sludge. These bioreactors were operated in batch mode at a temperature of 30-40°C (mesofilic condition) under anaerobic conditions. Operation period of the bioreactors is 90 days and methane percentage was monitored with a digital methane meter on a daily basis. At the end of the study, it was monitored that all of the seed sludges were partially effective on the anaerobic treatment of the organic fraction of municipal solid waste. COD reduction of 95% has been provided at the bioreactor including anaerobic seed sludge. But, anaerobic seed sludge has advantages related the to other seed sludges. Maximum methane percantage was (70%) and methane quantity (38,94 l) were monitored in the anaerobic seed sludge added bioreactor. Changes in the microbial population in leachates was detected by DGGE. Generally, Methanomicrobiales were observed abundantly in anaerobic seed sludge where Methanosarcinales were observed in Karahayıt sludge. But, Methanobacteriales were observed in Bio-one? seed sludge.

A new synthetic strategy for (R)- and (S)-3-hydroxy-4-(2,4,5-trifluorophenyl)butanoic acid, a building block in the preparation of sitagliptin and its derivatives, was developed. Pd(OAc)(2) catalyzed coupling of 2,4,5-trifluoro-1-iodobenzene with allyl alcohol gave 3-(2,4,5-trifluorophenyl)propanal in a yield of 95%. L-Proline catalyzed reaction of the 3-phenylpropanal (in only 1.2 molar equiv) with nitrosobenzene followed by reduction with NaBH4 and Pd/C catalyzed hydrogenation gave (R)-3-(2,4,5-trifluorophenyl) propane-1,2-diol with >99% ee and 65% yield. Selective tosylation of primary hydroxyl group of the 1,2-propandiol unit followed by cyanide displacement afforded (R)-3-hydroxy-4-(2,4,5-trifluorophenyl)butanenitrile (80%). The nitrile was converted to the title beta-hydroxy acid under basic hydrolysis in a yield of 90%. Thus, (R)-3-hydroxy-4-(2,4,5-trifluorophenyl)butanoic acid was prepared enantioselectively from the starting material in four steps and 45% overall yield. The reaction sequence was repeated with D-proline as the catalyst to give (S)-3-hydroxy-4-(2,4,5-trifluorophenyl)butanoic acid in 45% overall yield and >99% enantiomeric excess. (C) 2012 Elsevier Ltd. All rights reserved. Ministry of Science, Industry and Technology Republic of Turkey, FARGEM