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AASLD - TASL Connect Regional Meeting -- MAR 15-16, 2019 -- Istanbul, TURKEY WOS:000535263200004 PubMed: 32412901 Background/Aims: mbitasvir/paritaprevir/ritonavir (OMV/PTV/r) +/- dasabuvir (DSV) +/- ribavirin (RBV) combination has demonstrated excellent rates of sustained virologic response (SVR) and a very good safety profile in patients with the chronic hepatitis C virus (HCV) genotype 1 or 4 infections. We aimed to investigate the effectiveness and safety of OMV/PTV/r +/- DSV +/- RBV combination regimen in a real-world clinical practice. Materials and Methods: Data from HCV genotype 1 and 4 patients treated with OMV/PTV/r +/- DSV +/- RBV (n=862) in 34 centers across Turkey between April 1, 2017 and August 31, 2018 were recorded in a large national database. Demographic, clinical, and virologic data were analyzed. Results: The mean age of the patients was 55.63, and 430 patients (49.9%) were male. The majority had HCV genotype 1b infection (77.3%), and 66.2% were treatment-naive. Non-cirrhosis was present at baseline in 789 patients (91.5%). SVR12 rate was 99.1% in all patients. Seven patients had virologic failure. No significant differences were observed in SVR12 according to HCV genotypes. HCV RNA was undetectable at treatment week 4 in 90.9%, at treatment week 8 in 98.5%, and at the end of treatment (EOT) in 98.9%. SVR12 ratio was significantly higher in the non-cirrhotic patients compared to that in the compensated cirrhotic patients. Rates of adverse events (AEs) in the patients was 59.7%. Conclusion: The present real-life data of Turkey for the OBV/PTV/r +/- DSV +/- RBV treatment of patients with HCV genotype 1b, 1a, or 4 infection from 862 patients demonstrated high efficacy and a safety profile. AASLD, TASL

Bu çalışmada bazı biyolojik aktif 5,6-bis(4-sübstitüe fenil)-l,2,4-triazin -3-ol ve 5,6-bis(4-sübstitüe fenil)-l,2,4-triazin -3-tiyol türevlerinin asitlik sabitleri, sulu ortamda spektroskopik ve semi-empirik yöntemlerle incelenmiştir. İncelenen moleküllere, semiempirik AMI ve PM3 yöntemlerinin uygulanması ile bilgisayarda AHç AS değerleri hesaplanmıştır. Bileşiklerin asitlik sabitlerinin hesaplanmasında olası tautomerik formlar göz önüne alınmıştır. Teorik hesaplamalardan elde edilen verilerin, deneysel sonuçlarla uyumu araştırılmıştır. AMI ile hesaplanan ve deneysel olarak bulunan pKa değerleri arasında düşük bir koralasyon bulunmuş. Ancak PM3 ile hesaplanan pKa değerleri arasında iyi bir korelasyon gözlenmemiştir.Anahtar Kelimeler: 1,2,4-Triazin, tautomerik denge, konformasyon, asitlik bazlık(pKa), yan deneysel hesaplama, AMI, PM3 In this work acidity constants of some biologically active 5,6-bis(4-substituted phenyl)- 1,2,4-triazine -3-ol and 5,6-bis(4-substituted phenyl)- 1,2,4-triazine -3 -thiol derivates were studied in aqueous phase by spectroscopic and semi-empirical methods. AHf and AS values of investigated compounds were calculated by using semi- empirical AMI and PM3 methods. When the acidity constants of this compounds have been calculated possible tautomeric forms considered. The obtained values from theoretical calculations were evaluated by searching a possible correlation with the experimental results. A low correlation between the calculated AMI and experimental pKa values was obtained. But there wasn't a good correlation between the calculated PM3 and experimental pKa values.Keyword: 1,2,4-Triazine, tautomeric equilibrium, conformation, acidity and basicity (pKa), semi-empirical calculation, AMI, PM3 88

WOS: 000422764500003, PubMed ID: 29334931, Background: Nutmeg is the seed kernel inside the fruit of Myristica fragrans Houtt. (Myristicaceae). It possesses various pharmacological activities but is used in Cameroon only for its flavor in making cakes. The present study thus aimed to investigate the in vitro antibacterial activity and antibiotic modifying activities of crude seed kernel methanol extract (MFS), fractions (MFSa-e) as well as 3',4',7-trihydroxyflavone from Myristica fragrans against a panel of multi-drug resistant (MDR) Gram-negative bacteria. Methods: The modified rapid p-iodonitrotetrazolium chloride (INT) colorimetric assay was used to determine the Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) on the tested bacteria, as well as those of antibiotics in association with the extract and/or isolated compound. Column chromatography was used for the fractionation and purification of the seed kernel extract whilst the chemical structures of compounds were determined using spectroscopic techniques. Results: Phytochemical investigations lead to the isolation of 3',4',7-trihydroxyflavone from the fraction MFSb. The crude extract showed antibacterial activity with MICs ranging from 32 to 1024 mu g/mL on the majority of the 29 tested Gram-negative bacterial strains. Fraction MFSb inhibited the growth of 100% (29/29) of the tested bacterial strains, as well as the compound 3', 4', 7-trihydroxyflavone (12/12) with a MIC values ranging from 32 to 1024 mu g/mL, and 4 to 128 mu g/mL respectively. The lowest MIC value (4 mu g/mL) was recorded with 3', 4', 7-trihydroxyflavone against Providencia stuartii ATCC299645 as well as the best MBC value (16 mu g/mL) against the same strain. In the presence of Phenylalanine-Arginine-beta-Naphthylamide (PA beta N), an efflux pumps inhibitor, the activity of the extract increased on 73.33% (11/15) meanwhile that of 3',4',7-trihydroxyflavone increased on 100% tested bacteria. The compound 3',4',7-trihydroxyflavone potentiated the activity of antibiotics in the majority of the tested bacterial strains. Conclusion: The results of the present work provide additional information on the use of nutmeg and it major antibacterial component, 3',4',7-trihydroxyflavone, as a potential drug in the treatment of bacterial infections including multidrug resistant phenotypes., Scientific Research Projects Commission (SRPC) of Anadolu University, Eskisehir, Turkey [1306F110], Part of the research was funded by the Scientific Research Projects Commission (SRPC; Grant 1306F110) of Anadolu University, Eskisehir, Turkey.

Hastalıkların tedavisinde kullanılan ilaçlar hastalığın kaynağına göre (bakteri,virüs veya mantar) antibakteriyel, antiviral ve antifungal olarak adlandırılırlar.Antibakteriyel ajanları da içine alan antibiyotikler bakterilerin ve mantarların yol açtığıhastalıkların tedavisinde sıklıkla kullanılırlar. Ancak, 20. yüzyılın ortalarına doğru,antibiyotiklerin etkinliğinin düşmesine neden olan bakteri direncinin gelişmesi büyükbir sorun haline gelmiştir. Mevcut ilaçlara gösterilen bakteriyel dirençteki sürekli artışantibakteriyel tedavilerde ciddi bir sorundur ve yeni antibakteriyel ilaçlarınaraştırılmasını gerekli kılmıştır. 4-Kinolon çekirdek yapısına piyasada mevcut birçokantibakteriyel ajanın yapısında sıklıkla rastlanır. Bu çekirdek yapıda gerçekleştirileceken ufak yapısal modifikasyonlar çeşitli biyolojik aktivitelere sahip bileşiklerin eldesi ilesonuçlanabilmektedir.Ölümcül bakteriyel enfeksiyonların tedavisi için piyasada mevcut çok fazlaantibakteriyel ajan olsa da, bu ajanlara karşı gelişen direnç sebebiyle, yeni antibakteriyelajanlara duyulan ihtiyaçta orantılı olarak artmaktadır. Bu sebeple bu tez çalışmasında,benzotriazol kimyası kullanılarak sentezlenecek N-(2-aminoarilaçil)benzotriazoller ileçeşitli 1,3-dikarbonil bileşikleri arasındaki reaksiyondan, literatürde yer almayan yenibir yöntemle, bir 4-kinolon türevi olan 1-(4-hidroksi-2-alkil(aril)-3-kinolinil)etanonlarsentezlendi.Anahtar Sözcükler: 4-Kinolon, Benzotriazol, N-(2-Aminoarilaçil)benzotriazol, 1-(4-Hidroksi-2-alkil(aril)-3-kinolinil)etanon. The drugs used in the treatment of diseases are called antibacterial, antiviral andantifungal according to the source of the disease (bacteria, viruses, or fungi). Antibioticsthat contain antibacterial agents are often used for the treatment of diseases caused bybacteria and fungi. However, towards the middle of the 20th century, the development ofresistance to bacteria, which causes the effectiveness of antibiotics, has become a majorproblem. The continuous increase in bacterial resistance to existing drugs is a seriousproblem in antibacterial treatments and makes it necessary to search for newantibacterial drugs. 4-Quinolone core structure is frequently encountered in the structureof many marketed antibacterial agents. The smallest structural modifications to becarried out in this core structure may result in the acquisition of compounds havingvarious biological activities.Although there are too many antibacterial agents available on the market for thetreatment of deadly bacterial infections, due to the development of resistance to theseagents, the need for new antibacterial agents is increasing proportionately. Therefore, inthis thesis, 1-(4-hydroxy-2-alkyl (aryl) -3-quinolinyl) ethanones which are 4-quinolonederivatives were synthesized from the reaction between N-(2-aminoarylacyl)benzotriazole and various 1,3-dicarbonyl compounds, usingbenzotriazole chemistry.Keywords: 4-Quinolone, Benzotriazole, N-(2-Aminoarylacyl)benzotriazole, 1-(4-Hydroxy-2-alkyl(aryl)-3-quinolinyl)etanone. 72

Azotlu heterosiklik bileşikler tıp, eczacılık, biyomühendislik gibi alanlarda yaygın kullanıma sahip olduğundan dolayı oldukça önemli organik bileşiklerdir. Özellikle ilaç endüstrisinde ve tıbbi kimyada ilaç sentezi ve hastalıkların tedavisi için önemi büyüktür. Bu bileşiklerin sentezi ve biyolojik aktivitelerinin incelenmesi sentetik organik kimyacıların önemli çalışma konularından biridir.Kinazolon halkası yaklaşık 150 alkaloidin ve ilacın yapısında bulunur. Doğal olarak oluşan ve laboratuvar ortamında sentezlenen kinazolon türevleri antifungal, antimalaryal, antihiperlipidemik, antikonvülsant, antikanser gibi pek çok biyolojik ve farmakolojik etki göstermektedir.Bu tez çalışmasında, sübstitüe kinazolonlar N-(2-Aminobenzoil)benzotriazol bileşiklerinin amonyum asetat, çeşitli primer amin, hidrazid, ortoester ve aldehitler ile muamele edilmesi ile tek basamakta sentezlenmesi hedeflenmiştir. N-Heterocyclic compounds are very important organic compounds because they are widely used in medicine, pharmacy, bioengineering. Especially in the pharmaceutical industry and in medical chemistry, it is of great importance for drug synthesis and treatment of diseases. The synthesis of these compounds and the examination of their biological activity is one of the major study topics of synthetic organic chemists.The quinazolinone ring is present in the structure of about 150 alkaloids and drug. The naturally occurring and synthesized quinazolinone derivatives have many biological and pharmacological effects such as antifungal, antimalarial, antihyperlipidemic, anticonvulsant, anticancer.In this thesis, substituted quinazolinones are aimed to be synthesized in a one-pot reaction by treating the N-(2-aminobenzoyl)benzotriazole compounds with ammonium acetate, various primary amines, hydrazides, orthoesters and aldehydes. 135

WOS: 000440654100002, In this paper, we report a simple, low-cost, and environmentally friendly electrochemical method to obtain a novel copolymer consisting of l-pyrenyl-2,5-di(2-thienyl)pyrrole and pyrrole on a pencil graphite electrode (PGE). Poly(1-pyrenyl)-2,5-di(2-thienyl)pyrrole-co-pyrrole) that is P(PyrPy-co-Py) film was prepared by one-step potentiostatic codeposition in an ethanol solution containing PyrPy and Py monomers for supercapacitor applications. The electrodeposition of homopolymer and copolymer modified electrodes was carried out on the surface of the PGE via chronocoulometry. For comparison, P(Py)/PGE and P(PyrPy)/PGE were also electrochemically synthesized under the same reaction conditions. The surface morphologies of all the electrode materials were analyzed by field emission scanning electron microscopy. The capacitive properties of the modified PGEs were investigated in 1 M H2SO4 electrolyte solution by cyclic voltammetry, electrochemical impedance spectroscopy, and galvanostatic charge-discharge methods. Compared with P(Py)/PGE and P(PyrPy)/PGE, the P(PyrPy-co-Py)/PGE composite exhibited the best electrochemical behavior and had the highest specific capacitance value of 397. 18 F g(-1) in 1 M H-2 SO4 at a scan rate of 2 mV s(-1). These results indicated that this modified electrode can be used as an electrode material for electrochemical supercapacitors., Anadolu University Research Projects Commission [1401F016], Financial support from the Anadolu University Research Projects Commission (Project No.: 1401F016) is gratefully acknowledged.

WOS: 000403692800002, N-Substituted methyl 2-((azolyl)methyl)-3-arylacrylates were synthesized stereo- and regioselectively with one-pot reaction between Baylis-Hillman acetates and a suitable acylazole in the presence of K2CO3 as a base catalyst. The targeted N-substituted azole acrylates were efficiently obtained in good yields (39%-89%)., Anadolu University [1110F163], It is gratefully acknowledged that this work was supported financially by Anadolu University (Project No: 1110F163).

WOS: 000323936400008, A convenient and efficient method for the preparation of anthranilic esters and anthranilic thioesters has been developed by the treatment of N-(2-aminobenzoyl)benzotriazoles with alcohols and thiols in the presence of 4-(dimethylamino)pyridine (DMAP)., Anadolu University [1002F88], It is gratefully acknowledged that this work was supported financially by Anadolu University (Project No: 1002F88) and we are also grateful to AUBIBAM for providing 1H and 13C NMR spectra.

WOS: 000403998200011, A method for the preparation of 4-hydroxyquinoline-2,3-dicarboxylates has been developed by aza-Michael addition reaction of N-(2-aminobenzoyl)benzotriazoles with dimethyl acetylenedicarboxylate. 4-Hydroxyquinoline-2,3-dicarboxylates were obtained in moderate to good yields (53-87%), Anadolu University [1306F110], It is gratefully acknowledged that this work was supported financially by Anadolu University (Project No: 1306F110).

Tez (doktora) - Anadolu Üniversitesi, Anadolu Üniversitesi, Fen Bilimleri Enstitüsü, Kimya Anabilim Dalı, Kayıt no: 470562, Bu tez çalışmasında, 1-fenil-2,5-di(2-tiyenil)pirol, 9-fenantrenil-2,5-di(2-tiyenil)pirol, 1-pirenil-2,5-di(tiyenil)pirol ve 6-kraysenil-2,5-di(tiyenil)pirol olmak üzere dört farklı monomer kimyasal olarak sentezlenmiştir. Elde edilen moleküllerin karakterizasyonu 1H-NMR ve 13C-NMR spektroskopik yöntemleri ile gerçekleştirilmiştir. Monomerlerin pirol ile kopolimerleri ve polipirol elektrokimyasal olarak 0,1 M tetrabütilamonyum tetrafloroborat (TBABF4) katkı maddesi içeren etanol çözeltisi içerisinde kalem ucu grafit (KUG) çalışma elektrodu yüzeyinde kronokulometri (CC) yöntemi kullanılarak polimerleştirilmiştir. Tüm modifiye KUG elektrotların yüzey analizleri taramalı elektron mikroskopu (SEM) ile karakterize edilmiştir. Sentezi gerçekleştirilen iletken kopolimer ve polipirol modifiye KUG elektrotların kapasitif özellikleri 1 M sülfürik asit (H2SO4) elektrolit çözeltisinde dönüşümlü voltametri (CV), elektrokimyasal empedans spektroskopisi (EIS) ve galvanostatik şarj-deşarj (GCD) yöntemleri ile incelenmiştir. Elde edilen deneysel sonuçlara göre, modifiye KUG elektrotların kapasitans değerleri hesaplanmıştır. Kopolimerlerin, polipirol ile modifiye edilen KUG elektrotlar ile kıyaslandığında, daha iyi elektrokimyasal özelliklere ve daha yüksek kapasitans değerlerine sahip olduğu bulunmuştur.

WOS: 000267009400021, N-Protected dipeptidoylbeiizotriazoles react with aqueous ammonia to give dipeptide primary amides (77-98%) and with N-unprotected alpha-amino amides to afford tripeptide primary amides (82-86%).

WOS: 000383293300011, PubMed ID: 27267830, Ethnopharmacological relevance: Harungana madagascariensis Lam. ex Poir. (Hypericaceae) is used in folk medicine to treat a variety of human ailments, mainly antibacterial, antifungal, antiviral and viral infections. In the present study, the methanol extract from the leaves (HML) and bark (HMB) of this plant as well as fractions (HMBa-c), sub-fractions (HMBal-5) and compounds isolated from HMBa and HMBb namely betulinic acid (1), madagascin (2), ferruginin A (3) and Kaempferol-3-O-beta-D-glucopyranoside (4) were tested for their antimicrobial activities against a panel of 28 g-negative bacteria including multi drug resistant (MDR) phenotypes. Materials and methods: The broth microdilution method was used to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the above samples; column chromatography was used for the fractionation and purification of the bark extract whilst the chemical structures of compounds were determined using spectroscopic techniques. Results: Crude extract HMB together with fraction HMBa and sub-fraction HMBa3 were active on the 28 tested bacterial strains. HML as well as fractions HMBb, HMBc and sub-fractions HMBa1, HMBa2, HMBa4 and HMBa5 were selectively active. MIC values below or equal to 1024 mu g/mL were recorded with these samples on 92.9% (for HML and HMBa 4), 82.1% (for HMBb), 78.6% (for HMBa2), 50.0% (for HMBa5) and 42.9% (for HMBc) tested bacteria. For crude material, the lowest MIC value below 8 mu g/mL was obtained with HMB against Escherichia coli ATCC10536 and W3110 strains, and with sub-fraction HMBa3 against Klebsiella pneumoniae K2 strains. MIC values below 10 mu g/mL were recorded with compound 3 against E. coli ATCC10536, Enterobacter aerogenes ATCC13048 and EA294, Pseudomonas aeruginosa PA01, K. pneumoniae K2 and Kp55 and Enterobacter cloacae BM67. Conclusions: Harungana madagascariensis is a potential source of antimicrobial drugs to fight against MDR bacteria. The anthranol 3 is the main antibacterial constituents of the bark of the plant. HMB and compound 3 deserve further investigations to develop natural drug to combat Gram-negative bacteria and otherwise MDR phenotypes, Department of Chemistry, Anadolu University [1306F110], Authors are thankful to the Cameroon National Herbarium (Yaounde) for the plant identification. Authors are also thankful to UMR-MD1 (Mediterranean University, Marseille, France) for providing some clinical bacteria. Author would like to thank Department of Chemistry, Anadolu University for providing NMR spectra (project number: 1306F110).

WOS: 000372609000012, A novel and highly sensitive sensor based on poly[2, 5-di(2-thiophenyl)-1-p-(tolyl) pyrrole] was developed and successfully applied for the electrochemical determination of acetaminophen (AC) in pharmaceutical samples. The voltammetric behaviors of AC on modified pencil graphite electrode were investigated by cyclic voltammetry and differential pulse voltammetry in phosphate buffer solution. The voltammetric studies reveal that the polymer modified pencil graphite electrode possesses a remarkable electrocatalytic activity toward acetaminophen compared with the unmodified pencil graphite electrode. A linear dynamic range from 0.025 to 5 mu M and a correlation coefficient of 0.997 with a slope (sensitivity) of 23 mA M-1 were obtained for AC. The detection limit (S/N = 3) was determined as 1.94 nM, which shows a high sensitivity of the developed sensor for AC., Anadolu University Research Projects Commission [1401F016], This work was supported by the Anadolu University Research Projects Commission under Grant 1401F016.

WOS: 000251573700010, Reactions of readily available and stable N-(alpha-amidoalkyl)benzotriazoles 1 ( derived from a variety of aliphatic, aromatic or heterocyclic aldehydes) with diverse nitroalkanes, nitriles, alkynes and esters afforded N-(beta-nitroalkyl) amides 4 (54-96%), N-(beta-cyanoalkyl) amides 6 (58-88%), N- acylpropargylamines 11 (41-87%) and esters of beta-N-acylamino acids 13 (68-96%), respectively.

Tez (yüksek lisans) - Anadolu Üniversitesi, Anadolu Üniversitesi, Fen Bilimleri Enstitüsü, Kimya Anabilim Dalı, Kayıt no: 384210, Hem doğal hem de sentetik birçok bileşiğin yapısında sıklıkla karşılaşılan azoller heterosiklik bileşiklerin önemli bir sınıfını oluştururlar. Antifungal, antibakteriyel, antidiyabetik, antitümör ve daha birçok terapötik etki gösterdikleri için azolleri içeren organik bileşiklerin sentezi ilaç kimyasındaki en önemli hedeflerden biridir. Günümüze kadar, imidazol, benzimidazol ve benzotriazol gibi azolleri içeren birçok ilaç geliştirilmiştir. Bu ilaçlar, sahip oldukları çok çeşitli biyolojik aktivitelerden dolayı kanserden AIDS'e, kalp rahatsızlıklarından ülsere kadar birçok hastalığın tedavisinde rahatlıkla kullanılmaktadırlar. Azolleri içeren bileşiklerin yüksek farmakolojik aktivite göstermeleri ve Baylis-Hillman ürünlerinin farklı fonksiyonelliğe sahip bileşiklerin hazırlanmasında uygun bir platform sunması sebebiyle bu tez çalışmasında N-açilazoller kullanılarak çeşitli N-sübstitüe azolakrilatların sentezi hedeflendi. İlk olarak, bir aldehit ile metil akrilatın çözücüsüz ortam kullanılarak, başarılı bir katalizör olan 1,4-diazabisiklo[2.2.2]oktan (DABCO) varlığında reaksiyona sokulmasıyla başlangıç maddesi olan Baylis-Hillman ürünleri elde edildi. Daha sonra, N-açilazoller ve Baylis-Hillman ürünleri arasındaki reaksiyondan literatüre alternatif oluşturacak yeni bir yöntemle potasyum karbonat katalizörlüğünde çeşitli N-sübstitüe azolakrilatların sentezi gerçekleştirildi. Elde edilen bileşiklerin yapıları 1H-NMR ve 13C-NMR spektrumları yardımı ile aydınlatıldı. Elde edilen sonuçlar elementel analiz sonuçları ile desteklendi.

WOS: 000363828500022, 2-Substituted quinolone 3-carboxylates were obtained in moderate to good yields by the reaction of N-(2-aminobenzoyl)benzotriazoles with beta-ketoesters in the presence of t-BuOK in THF, Anadolu University [1306F110], This work is dedicated to Professor Alan Roy Katritzky, who died on 10th February, 2014. It is gratefully acknowledged that this work was supported financially by Anadolu University (Project No: 1306F110).

Tez (yüksek lisans) - Anadolu Üniversitesi, Anadolu Üniversitesi, Fen Bilimleri Enstitüsü, Kimya Anabilim Dalı, Kayıt no: 382175, Bu tez çalışmasında, ısıl yalıtımda kullanmak amacıyla sert poliüretan köpük malzeme elde edilmesi amaçlanmıştır. Bu doğrultuda ilk olarak, başlatıcı ve propilen oksit, bir katalizör eşliğinde tepkimeye sokularak polieter poliol sentezlenmiştir. Polieter poliol sentezinin optimizasyonu gerçekleştirilmiş ve sentezlenen poliolün karakterizasyonu Fourier Transform Infrared Spektrofotometresi (FT-IR), jel geçirgenlik kromatografisi (GPC) ve hidroksil sayısı tayini (ASTM E 1899) ile yapılmıştır. Sentezlenen poliol tek atış tekniği ile izosiyanatla (Difenilmetan-4,4'-diizosiyanat) tepkimeye sokularak sert poliüretan köpük elde edilmiştir. Elde edilen sert poliüretan köpüğün fiziksel ve mekanik özelliklerini inceleme amacıyla, taramalı elektron mikroskobu analizi (SEM), ısıl iletkenlik ölçümü, sıkışma dayanımı testi, açık kapalı hücre oranının ölçümü ve köpük testi gerçekleştirilmiştir.

Tez (doktora) - Anadolu Üniversitesi, Anadolu Üniversitesi, Fen Bilimleri Enstitüsü, Kimya Anabilim Dalı, Kayıt no: 1035719, Bakterilerin, bitkilerin ve hayvanların temel biyokimyasal reaksiyonlarında ara ürün olarak ortaya çıkanantranilik asit, doğada yaygın olarak bulunan birçok bileşiğin de başlangıç maddesidir. Bu bileşikler arasında alkaloitler, DIMBOA gibi bitki sinyalizasyon bileşikleri ve indol-3-asetik asit bulunur. Aynı zamanda, antranilik asitin ester, tiyoester ve amit türevleri sentetik organik kimyada çeşitli heterosikliklerin sentezinde yaygın olarak kullanılırlar. Antranilik asitin doğada yaygın olarak bulunması ve türevlerinin sentetik süreçlerdeki işlevselliği, antranilik asit türevlerinin sentezinde kullanılabilecek daha kullanışlı yeni yöntemlerin ve reaktiflerin geliştirilmesi ihtiyacını ortaya koymaktadır. NAsilbenzotriazoller ise, uzunyıllardır asilleme ajanı olarak kullanılan bileşiklere alternatif olarak, esterlerin, tiyoesterlerin ve amitlerin sentezinde daha ılımlı reaksiyon şartları sunmaktadır. Bu amaçla bu tez çalışmasında öncelikli olarak, benzotriazol metodolojisi kullanılarak, antranilik asit, benzotriazol ve DCC arasındaki reaksiyondan tamamı yeni N-(2-aminoarilasil)benzotriazoller sentezlendi. Sonrasında, antranilik asit esterleri, tiyoesterleri ve amitleri, literatür yöntemlerinden farklı yeni bir yöntemle, N-(2-aminoarilasil)benzotriazollerin çeşitli alkol, tiyoalkol ve aminlerle muamele edilmesinden yüksek verimlerle elde edildi. Sentezlenen bileşiklerin yapıları çeşitli spektroskopik yöntemlerle aydınlatılmıştır.

Tez (yüksek lisans) - Anadolu Üniversitesi, Anadolu Üniversitesi, Fen Bilimleri Enstitüsü, Kimya Anabilim Dalı, Kayıt no: 384251, Heterosiklik maddeler tıp, eczacılık ve kimyada geniş uygulama alanına sahip olduğundan dolayı, bu maddeler sentetik organik kimyanın bir parçası olmuştur. İlaç keşfinde seçkin yapılar olarak heterosiklik maddelerin araştırılması, ilaç kimyasında önemli alanlardan biridir. Bu seçkin yapılar yüksek bağlanma yeteneğine sahip çeşitli reseptörler için ligand olarak davranan bir molekül sınıfını temsil eder. Bu moleküllerin keşfi, ilaç kimyasında biyolojik olarak aktif yeni maddelerin sentezlenmesinde büyük öneme sahiptir. Bu tez çalışmasında, aldehit ve akrilonitrilin DABCO katalizörlüğünde reaksiyonu ile 2-(hidroksiarilalkil)akrilonitriller oda sıcaklığında hazırlandı. Elde edilen 2-(hidroksiarilalkil)akrilonitriller oda sıcaklığında N-asetil benzotriazol ve N-asetil benzimidazol ile tepkimeye sokularak N-sübstitüe 2-((benzotriazol-il)metil)-3-akrilonitriller ve N-sübstitüe 2-((benzimidazol-il)metil)-3-akrilonitriller sentezlenmiştir.

WOS: 000262033000042, Various beta '-amido-beta-diketones were first synthesized with N-(alpha-amidoalkyl)benzotriazole-mediated amidoalkylation of 1,3-diketones in moderate yields. These intermediates undergo rapid condensation with hydrazines to give the corresponding N-[beta-(3,5-di and 1,3,5-trisubstituted pyrazol-4-yl)alkyl]amides

WOS: 000247311100009, Novel syntheses of beta-thioamido ketones via thioamidoalkylations of malonates, beta-keto esters, beta-diketones, enol silyl ethers, and enamines with N-(alpha-thioamidoalkyl)benzotriazoles are described.

WOS: 000392349100003, PubMed ID: 28061888, Background: Elaeophorbia drupifera (Thonn.) Stapf. (Euphorbiaceae) is used in Cameroonian folk medicine to treat several ailments including bacterial-related diseases such as skin infections. In this study, the methanol extract from the leaves (EDL), fractions (EDLa-d), sub-fractions EDLc1-7 and EDLc31-35 as well as isolated compounds were tested for their antimicrobial activities against a panel of Gram-negative and Gram-positive bacteria including multidrug resistant (MDR) phenotypes. Methods: The broth microdilution method was used to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the above samples; column chromatography was used for the fractionation and purification of the leaves extract whilst the chemical structures of compounds were determined using spectroscopic techniques. Results: Phytochemical investigation lead to the isolation of a mixture (1: 3) of stigmasterol and beta-sitosterol (1 + 2), euphol (3), sitosterol-O-beta-D-xylopyranoside (4), 3,3', 4'-tri-O-methylellagic acid (5), a mixture (1: 1) of afzelin and quercetin-3-O-beta-D-xylopyranoside (6 + 7), 3,3', 4'-tri-O-methylellagic acid 4-O-beta-D-glucopyranoside (8), ellagic acid-4-O-beta- xylopyranoside-3,3', 4'-trimethyl ether (9) from EDLc. Crude extract and fractions displayed selective activities with MIC values ranged from 32 to 1024 mu g/mL for EDL against 84.9% of the 33 tested bacteria, 93.9% for EDLc, 69.7% for EDLb, 33.4% for EDLa and 0.03% for EDLd. MIC values ranged from 16 to 1024 mu g/mL were obtained with EDLc3 and EDLc4 on all tested bacteria meanwhile other sub-fractions displayed selective activities. MIC value of 32 mu g/mL was obtained with fractions EDLa against Escherichia coli AG100, EDLc against Enterobacer aerogenes ATCC13048 and EA298. For sub-fractions obtained from EDLc, the lowest MIC value of 16 mu g/mL was recorded with EDLc3 against Staphylococcus aureus MRSA11. A corresponding value of 8 mu g/mL against Providencia stuartii NAE16 was recorded with EDLc33 obtained from further fractionation of EDLc3. EDLc3 had MIC values below 100 mu g/mL against all tested bacteria. Compound 5 as well as the mixture (1: 1) of 6 and 7 inhibited the growth of all the tested bacteria with MICs ranged from 64 to 256 mu g/mL. Conclusion: Elaeophorbia drupifera is a potential source of phytomedicine to tackle MDR bacteria. Sub-fraction EDLc3 was more active than all isolated compounds and deserves further investigations to develop natural drug to combat Gram-negative, Gram-positive bacteria and otherwise MDR phenotypes., Department of Chemistry, Anadolu University [1306F110], Authors are thankful to the Cameroon National Herbarium (Yaounde) for the plant identification. Authors are also thankful to UMR-MD1 (Mediterranean University, Marseille, France) for providing some clinical bacteria. Author would like to thank Department of Chemistry, Anadolu University for providing NMR spectra (project number: 1306F110).