Yazar "Şahin, Zafer" için listeleme
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Antimicrobial evaluation of trisubstituted 2-piperazinyl thiazoles
Giray, Betül; Yurttaş, Leyla; Şahin, Zafer; Berk, Barkın; Demirayak, Şeref (İstanbul Medipol University, 2019)Thiazole and basic nitrogen containing rings are important chemical moieties of antimicrobial drugs. In recent, third generation cephalosporins include thiazole ring system. In this study, we synthesized 33 piperazine ... -
Design and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors
Şahin, Zafer; Biltekin, Sevde Nur; Bülbül, Emre Fatih; Yurttaş, Leyla; Berk, Barkın; Demirayak, Şeref (Taylor & Francis Ltd, 2020)Newly synthesized 4-substituted phenyl-2-(4-substituted phenylpiperazine-1-yl)thiazole derivatives (4a-v) were evaluated in terms of their acetylcholinesterase (AChE) inhibition activities. Twenty-two compounds were tested ... -
Discovery of novel potent human chondrosarcoma (SW1353) inhibitors: 4-(2/3/4-pyridyl)thiazole 2-acetamide derivatives
Coşkun, Göknil Pelin; Şahin, Zafer; Erdoğan, Ömer; Çevik, Özge; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Ülgen, Mert; Demirayak, Şeref (Elsevier B.V., 2023)Chondrosarcoma is the most common cartilage sarcoma among adult patients. It is mainly observed after the degradation of chondrocytes in the case of cell stress. Unfortunately, the mortality among patients is high as a ... -
Evaluation of apoptosis pathway of geraniol on ishikawa cells
Kuzu, Betül; Cüce, Gökhan; Çınar Ayan, İlknur; Gültekin, Burcu; Canbaz, Halime Tuba; Dursun, Hatice Gül; Şahin, Zafer; Keskin, İlknur; Kalkan, Sabiha Serpil (Routledge, 2021)Endometrial cancer is the most common type of cancer in the female reproductive system. Geraniol is acyclic monoterpene alcohol derived from essential oils of aromatic plants. This study aimed to investigate the apoptosis ... -
Importance and review of drug metabolite synthesis
Şahin, Zafer; Omurtag Özgen, Pınar Sinem; Rollas, Sevim (Istanbul University, 2023)Phase I and Phase II metabolic reactions are involved in the pharmacokinetic properties of drugs after administration. These reactions mainly aim to make drugs more polar and eliminate them safely. However, some of these ... -
Molecular modelling and activity analysis of mycobacterium tuberculosis DNA gyrase B ATPase active site
Berk, Barkın; Şahin, Zafer (University of Istanbul, 2017)Computer-based algorithms and statistical techniques such as receiver operating characteristic (ROC) curves are increasingly used for the design of new ligands. X-ray crystallographic data and homology models allow examining ... -
Novel benzofurane carbonyl analogs of donepezil as acetylcholinesterase inhibitors
Şahin, Zafer; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Küçükkılınç, Tuba Tüylü; Demirayak, Şeref (Elsevier B.V., 2022)Donepezil is the most prescribed drug for mild to moderate Alzheimer's Disease. There is not any alternative drug with this potency yet. New scaffolds bearing benzofurans and amines are being tested for good potency on ... -
Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation
Şahin, Zafer; Özhan, Yağmur; Sipahi, Hande; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Demirayak, Şeref (Walter de Gruyter GmbH, 2022)Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with alpha-hydroxy ... -
Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition
Şahin, Zafer; Biltekin, Sevde Nur; Yurttaş, Leyla; Berk, Barkın; Özhan, Yağmur; Sipahi, Hande; Gao, Zhanguo; Jacobson, Kenneth A.; Demirayak, Şeref (Elsevier France-Editions Scientifiques Medicales Elsevier, 2021)Thiouracil and thiocytosine are important heterocyclic pharmacophores having pharmacological diversity. Antitumor and antiviral activity is commonly associated with thiouracil and thiocytosine derivatives, which are well ... -
Novel thiazole-piperazine derivatives as potential cholinesterase inhibitors
Demirayak, Şeref; Şahin, Zafer; Ertaş, Merve; Bülbül, Emre Fatih; Bender, Ceysu; Biltekin, Sevde Nur; Berk, Barkın; Sağlık, Begüm Nurpelin; Levent, Serkan; Yurttaş, Leyla (Wiley, 2019)Dementia is a cognitive disorder mostly associated with Alzheimer's disease (AD) in addition to being seen in many other diseases of the central nervous system (CNS). The limited number of drugs is not sufficient to provide ... -
Potent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives
Ertaş, Merve; Şahin, Zafer; Bülbül, Emre Fatih; Bender, Ceysu; Biltekin, Sevde Nur; Berk, Barkın; Yurttaş, Leyla; Nalbur, Aysu M.; Çelik, Hayati; Demirayak, Şeref (Wiley, 2019)The antioxidant, antimalarial, antibacterial, and antitumor activities of thiosemicarbazones have made this class of compounds important for medicinal chemists. In addition, thiosemicarbazones are among the most potent and ... -
Pyridine-substituted thiazolylphenol derivatives: Synthesis, modeling studies, aromatase inhibition, and antiproliferative activity evaluation
Ertaş, Merve; Şahin, Zafer; Berk, Barkın; Yurttaş, Leyla; Biltekin, Sevde Nur; Demirayak, Şeref (Wiley-VCH Verlag, 2018)Drugs used in breast cancer treatments target the suppression of estrogen biosynthesis. During this suppression, the main goal is to inhibit the aromatase enzyme that is responsible for the cyclization and structuring of ... -
Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives
Şahin, Zafer; Ertaş, Merve; Berk, Barkın; Biltekin, Sevde Nur; Yurttaş, Leyla; Demirayak, Şeref (Pergamon-Elsevier Science Ltd, 2018)Steroidal and non-steroidal aromatase inhibitors target the suppression of estrogen biosynthesis in the treatment of breast cancer. Researchers have increasingly focused on developing non-steroidal derivatives for their ... -
Synthesis and antibacterial evaluation of novel benzimidazole, benzothiazole, benzofurane, and naphtofurane derivatives of aminothiazoles
Şahin, Zafer; Tok, Büşra Işıl; Akgün, Erol; Çaşkurlu, Ayşegül; Yurttaş, Leyla; Berk, Barkın; Demirayak, Şeref (Ankara Association of Pharmaceutical Sciences, 2022)The thiazole ring is the core of bioactive molecules that generate broad activity. These activities include anticonvulsant, antimicrobial, antituberculosis, antiviral, etc. In this work, starting from seconder/cyclic amines, ... -
Synthesis and antimicrobial activity evaluation of novel nitrofuranthiazoles
Yurttaş, Leyla; Şahin, Zafer; Er, Sevda; Demirayak, Şeref (University of Istanbul, 2016)In this work, six novel 4-aryl-2-[2-((5-nitrofuran-2-yl)methylene)hydrazinyl] thiazole derivatives (2a-f) were synthesized starting from 5-nitro-2-furaldehyde diacetate by using Hantzsch thiazole synthesis. The antimicrobial ... -
Synthesis and in vitro antitumor activities of novel thioamide substituted piperazinyl-1,2,4-triazines
Şahin, Zafer; Biltekin, Sevde Nur; Ozansoy, Mehmet; Hemiş, Bervis; Yurttaş, Leyla; Berk, Barkın; Demirayak, Şeref (Wiley, 2022)Triazines are in great interest for their potential to mimic nucleoside analog compounds. Three different isomers exist including 1,2,3-triazine, 1,3,5-triazine (s-triazine) and 1,2,4-triazine. All of these skeletons were ... -
Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents
Yurttaş, Leyla; Şahin, Zafer; Çiftçi Akalın, Gülşen; Temel Edip, Halide; Demirayak, Şeref (University of Istanbul, 2016)In this study, new 3, 5, 6-trisubstituted 1, 2, 4-triazine derivatives (1-9) were synthesized and their structures were determined by using NMR, IR and Mass spectroscopic methods. In vitro antitumor activities against MCF-7 ... -
Synthesis, antioxidant and antimicrobial properties of novel pyridyl-carbonyl thiazoles as dendrodoine analogs
Şahin, Zafer; Biltekin, Sevde Nur; Yurttaş, Leyla; Demirayak, Şeref (Scientific and Technical Research Council of Turkey, 2020)Marine compound dendrodoine was first obtained from tunicate species (Dendrodo grossularia). It has a five-membered ring, namely, it is a heterocycle thiadiazole, which is found rarely in natural sources. Following its ... -
Synthesis, characterization and antibacterial evaluation of new pyridyl-thiazole hybrids of sulfonamides
Şahin, Zafer; Biltekin, Sevde Nur; Yurttaş, Leyla; Demirayak, Şeref (Istanbul University, 2021)Background and Aims: Sulfonamide drugs are a very old and noted group of small molecules, and are still one of the most important antimicrobial compounds. In this study, starting from sulfonamide drugs, new original compounds ... -
Synthesis, characterization, COX1/2 inhibition and molecular modeling studies on novel 2-thio-diarylimidazoles
Şahin, Zafer; Koçoğlu Kalkan, Melike; Berk, Barkın; Yurttaş, Leyla; Bender, Ceysu; Biltekin Kaleli, Sevde Nur; Demirayak, Şeref (Scientific Technical Research Council Turkey-Tubitak, 2021)Heterocyclic compounds with diaryl substituents have been a milestone approach for selective cyclooxygenase 2 (COX 2) inhibition by bioisosteric replacements and modifications. It is also known that thiazole derivatives ...