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Novel benzydamine hydrochloride and chlorhexidine gluconate loaded bioadhesive films for local treatment of buccal infections
Arpa, Muhammet Davut; Yağcılar, Ayşe Pınar; Biltekin, Sevde Nur (Editions de Sante, 2023)Benzydamine hydrochloride (BZD), chlorhexidine gluconate (CHG) or their combination are frequently used as liquid dosage forms for the local treatment of buccal fungal and bacterial infections. However, the short residence ... -
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 sprayable thermosensitive benzydamine hydrogels for topical application: Development, characterization, and in vitro biological activities
Arpa, Muhammet Davut; Kesmen, Ebrar Elif; Biltekin, Sevde Nur (Springer Science and Business Media Deutschland GmbH, 2023)Benzydamine hydrochloride (BZD) having analgesic, anesthetic, and anti-inflammatory effects is used orally or topically in the treatment of disorders such as joint inflammation and muscle pain. Within the scope of this ... -
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 ... -
Separate and mutual effects of BIRB796 and bortezomib on pHsp27 and viability of U87MG glioma cells
Biltekin, Sevde Nur; Önay Uçar, Evren (Pleiades Publishing, 2023)Hsp27 phosphorylation is associated with many pathways in glioma, such as tumor cell proliferation and apoptosis inhibition. The aim of this study is to examine the separate and mutual effects of BIRB796 and bortezomib on ... -
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 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 some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activity
Ertaş, Merve; Biltekin, Sevde Nur; Berk, Barkın; Yurttaş, Leyla; Demirayak, Şeref (Taylor & Francis Ltd, 2022)Within this study, 20 2-[(5,6-diaryl-1,2,4-triazin-3-yl)thio]-N-(benzo/thiazol-2-yl)acetamide derivatives (4a-4t) were synthesized and COX inhibitory activities of the compounds were investigated. Compounds 4k-4o, which ... -
Synthesis, antimicrobial activity studies and molecular property predictions of schiff bases derived from ortho-vanillin
Berk, Barkın; Ertaş, Merve; Biltekin, Sevde Nur (University of Istanbul, 2017)Schiff bases are known to possess anticancer, antibacterial, antifungal, antitubercular, anti-inflammatory, antibacterial and antimalarial properties. At the same time, in recent years, prediction of drug-likeness, molecular, ... -
The synthesis, antimicrobial activity studies, and molecular property predictions of novel benzothiazole-2-thione derivatives
Berk, Barkın; Atlas Tahirovic, Yeşim; Bülbül, Emre Fatih; Biltekin, Sevde Nur (University of Istanbul, 2017)Benzothiazoles and 2-mercaptobenzothiazoles are important classes of bioactive organic scaffolds possessing antibacterial, antifungal, antitubercular, antiinflamma-tory, antidiabetic, and antimalarial properties. In recent ... -
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 ... -
Thiazole-substituted benzoylpiperazine derivatives as acetylcholinesterase inhibitors
Şahin, Zafer; Ertaş, Merve; Bender, Ceysu; Bülbül, Emre Fatih; Berk, Barkın; Biltekin, Sevde Nur; Yurttaş, Leyla; Demirayak, Şeref (Wiley, 2018)Hit, Lead & Candidate Discovery After acetylcholine is released into the synaptic cleft, it is reabsorbed or deactivated by acetylcholinesterase (AChE). Studies on Alzheimer's disease (AD) in the mid-20th century proved ...