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Öğe Coumarin or benzoxazinone based novel carbonic anhydrase inhibitors synthesis molecular docking and anticonvulsant studies(Journal of Enzyme Inhibition and Medicinal Chemistry, 2016) Karataş, Mert Olgun; Uslu, Harun; Sarı, Suat; Alagöz, Mehmet Abdullah; Karakurt, Arzu; Alıcı, Bülent; Bilen, Çiğdem; Yavuz, Emre; Gençer, Nahit; Arslan, OktayAmong many others, coumarin derivatives are known to show human carbonic anhydrase (hCA) inhibitory activity. Since hCA inhibition is one of the underlying mechanisms that account for the activities of some antiepileptic drugs (AEDs), hCA inhibitors are expected to have antiseizure properties. There are also several studies reporting compounds with an imidazole and/or benzimidazole moiety which exert these pharmacological properties. In this study, we prepared fifteen novel coumarin-bearing imidazolium and benzimidazolium chloride, nine novel benzoxazinone-bearing imidazolium and benzimidazolium chloride derivatives and evaluated their hCA inhibitory activities and along with fourteen previously synthesized derivatives we scanned their anticonvulsant effects. As all compounds inhibited purified hCA isoforms I and II, some of them also proved protective against Maximal electroshock seizure (MES) and ScMet induced seizures in mice. Molecular docking studies with selected coumarin derivatives have revealed that these compounds bind to the active pocket of the enzyme in a similar fashion to that previously described for coumarin derivatives.Öğe Dual effect of coumarin benzimidazolium ionic salt covalently bonded on a silica network(SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2015) Gültek, Ahmet; Aksüt, Davut; Seçkin, Turgay; Birhanlı, Emre; Karataş, Mert Olgun; Alıcı, BülentSynthesis of the ionic liquid 1-allyl-3-(4-methyl-7,8-dihydroxy-2H-chromen-2-one) benzimidazolium chloride followed by the conversion of ammonium salts on the imidazole ring hooked to the coumarin group was modified by postmodification of the silica matrix where 3-chloropropyltrimethoxysilane was used as not only a surface modification agent, but also as an ATRP halogen source. The synergetic effect of charged ammonium groups as well as hydroxyl groups present on the coumarin was investigated in terms of ATRP polymerization. The results confirmed that brush polymers show outstanding antibacterial effects against Escherichia colt, Staphylococcus aureus, and Pseudomonas aeruginosa.Öğe Functionalized imidazolium and benzimidazolium salts as paraoxonase 1 inhibitors synthesis characterization and molecular docking studies(Bioorganic & Medicinal Chemistry, 2016) Karataş, Mert Olgun; Uslu, Harun; Alıcı, Bülent; Gökçe, Başak; Gençer, Nahit; Arslan, Oktay; Arslan, Nahide Burcu; Özdemir, NamıkParaoxonase (PON) is a key enzyme in metabolism of living organisms and decreased activity of PON1 was acknowledged as a risk for atherosclerosis and organophosphate toxicity. The present study describes the synthesis, characterization, PON1 inhibitory properties and molecular docking studies of functionalized imidazolium and benzimidazolium salts (1a–5g). The structures of all compounds were elucidated by IR, NMR, elemental analysis and structures of compounds 2b and 2c were characterized by single-crystal X-ray diffraction. Compound 1c, a coumarin substituted imidazolium salt showed the best inhibitory effect on the activity of PON1 with good IC50 value (6.37 lM). Kinetic investigation was evaluated for this compound and results showed that this compound is competitive inhibitor of PON1 with Ki value of 2.39 lM. Molecular docking studies were also performed for most active compound 1c and one of least active compound 2c in order to determine the probable binding model into active site of PON1 and validation of the experimental results.Öğe Some coumarins and benzoxazinones as potent paraoxonase 1 inhibitors(Journal of Enzyme Inhibition and Medicinal Chemistry, 2016) Karataş, Mert Olgun; Alıcı, Bülent; Gökçe, Başak; Gencer, Nahit; Arslan, Oktay; Uslu, HarunIn this study, we aimed to investigate the effect of some coumarin and benzoxazinone derivatives on the activity of human PON1. Human serum paraoxonase 1 was purified from fresh human serum blood by two-step procedures that are ammonium sulfate precipitation (60–80%) and then hydrophobic interaction chromatography (Sepharose 4B, L-tyrosine and 1-napthylamine). The enzyme was purified 232-fold with a final specific activity of 27.1 U/mg. In vitro effects of some previously synthesized ionic coumarin or benzoxazinone derivatives (1–21) on purified PON1 activity were investigated. Compound 14 (1-(2,3,4,5,6)-pentamethylbenzyl-3-(6,8-dimethyl-2H-chromen-2-one-4-yl))benzimidazolium chloride was found out as the strongest inhibitor (IC50 ¼ 7.84 mM) for PON1 among the compounds. Kinetic investigation and molecular docking study were evaluated for one of the most active compounds (compound 12) and obtained data showed that this compound is competitive inhibitor of PON1 and interact with Leu262 and Ser263 in the active site of PON1. Moreover, coumarin derivatives were found out as the more potent inhibitors for PON1 than benzoxazinone derivativesÖğe Synthesis, Characterization, and Carbonic Anhydrase Inhibitory Properties of Silver(I) Complexes of Benzimidazole Derivatives(2019) Karataş, Mert Olgun; Ergün, AdemAbstract: The antimicrobial properties of silver compounds and biological properties ofbenzimidazole derivatives have been well known for many years. In the present study, in terms oftheir biological potential, six novel silver(I)-N-alkylbenzimidazole derivatives were synthesized inorder to examine their carbonic anhydrase (CA) inhibitory properties. All complexes werecharacterized by the combination of 1H NMR, 13C NMR, mass, FT-IR spectroscopic methods andelemental analyses. The inhibitory properties of all complexes were tested on the esterase activityof human CA I and II (hCA I and hCA II). Acetazolamide was used as a standard. All complexesinhibited the hCA I and hCA II activity in the range of 27.37-29.58 µM and 20.93-27.25 µM,respectively.Öğe Yeni kumarin bileşiklerinin sentezi, karakterizasyonu ve özelliklerinin incelenmesi(İnönü Üniversitesi, 2017) Karataş, Mert OlgunKumarin bileşikleri çeşitli biyolojik aktiviteleri nedeni ile kimya ve tıp alanlarında ilgi ile araştırılmaktadır. En çok bilinen özellikleri anti-koagülant özellik göstermeleridir. Bunun yanında anti-HIV, anti-mikrobiyal ve anti-kanser özelliklerine ait çalışmalar son yıllarda hız kazanmıştır. Biyolojik özelliklerine ek olarak floresans özelliklerinden dolayı bazı kumarin türevleri endüstride boyar madde olarak kullanılmaktadır. Arduengo tarafından ilk serbest ve kararlı N-heterosiklik karbenin (NHC) izole edilmesinden sonra NHC kompleksleri üzerinde çok sayıda çalışmalar yapılmıştır. Günümüzde metal-NHC komplekslerinin organometalik kimyada katalizör olarak önemli bir yeri vardır. Bunun yanında son yıllarda yapılan çalışmalar ile metal-NHC komplekslerinin farmasotik özellikleri de önem kazanmaktadır. Bu bilgiler ışığında, kumarin grubu içeren Ag(I)-, Rh(I)- ve Ir(I)-NHC komplekslerinin sentezi ve karakterizasyonu gerçekleştirilip özellikleri incelenmiştir. Bu tez kapsamında yapılan çalışmalar yedi başlık altında özetlenebilir; 1) Sekiz adet 1-alkil-3-kumarin imidazolyum (2a-h) ve on üç adet 1-alkil-3-kumarin benzimidazolyum tuzu (2i-v) sentezlenmiş ve uygun spektroskopik yöntemler ile karakterize edilmiştir. 2) Kumarin içeren sekiz adet Ag(I)-NHC kompleksi (3a-h) sentezlenmiş ve uygun spektroskopik yöntemler ile karakterize edilmiştir. 3) Kumarin içeren on dokuz adet Rh(I)-NHC kompleksi (4a-t) sentezlenmiş ve uygun spektroskopik yöntemler ile karakterize edilmiştir. 4) Kumarin içeren dokuz adet Ir(I)-NHC kompleksi (5a-i) sentezlenmiş ve uygun spektroskopik yöntemler ile karakterize edilmiştir. 5) Sentezlenen Ag(I)-NHC kompleksleri ve karşılık gelen azolyum tuzlarının Staphylococcus aureus ve Enterococcus faecalis (Gram-pozitif), Escherichia coli ve Pseudomonas aeruginosa (Gram-negatif) bakteri ve Candida albicans ve Candida tropicalis mantar türlerine karşı anti-mikrobiyal etkileri incelenmiştir. 6) Sentezlenen Rh(I)-NHC komplekslerinin fenilasetilenin hidrofosfinasyonu tepkimesinde katalitik özellikleri incelenmiştir. 7) Sentezlenen Ir(I)-NHC komplekslerinin alkinlerin hidrosilasyonu tepkimesinde katalitik özellikleri incelenmiştir.Öğe Yeni N-benzilbenzimidazol-gümüş(I) komplekslerinin sentezi, karakterizasyonu, karbonik anhidraz ve polifenol oksidaz enzimleri üzerindeki inhibitör özellikleri(2020) Ergün, Adem; Karataş, Mert OlgunGümüş komplekslerinin biyolojik özellikleri çok iyi bilinmesine rağmen enzim inhibisyonu özelliklerine yönelik çalışmalar oldukça sınırlıdır. Diğer taraftan benzimidazol türevlerinin anti-kanser etki mekanizmalarından birinin enzim inhibisyonu olduğu bilinmektedir. Bu nedenle bu çalışmada, beş yeni N-benzilbenzimidazol-gümüş(I) kompleksi sentezlendi, 1H NMR, 13C NMR, IR ve kütle spektroskopik yöntemleri ve elementel analiz sonuçları ile tamamen karakterize edildi. Elde edilen komplekslerin insan karbonik anhidraz I - II ve polifenol oksidaz enzimleri üzerindeki inhibisyon etkileri incelendi ve komplekslerin bu enzimlerin aktivitelerini sırasıyla 29.58-32.65 ?M, 21.05-23.65 ?M ve 30.38-44.45 ?M’lık IC50 değerleri ile inhibe ettiği gözlendi. Gümüş bileşiklerinin insan vücudunda düşük konsantrasyonlarda toksik etki göstermediği de göz önüne alınırsa, bu çalışmada test edilen kompleksler karbonik anhidraz inhibitörü olarak glokom tedavisinde ve polifenol oksidaz inhibitörü olarak ise hiper-pigmentasyon hastalığı tedavisinde kullanılmak için umut verici adaylardır.