Zeynep Özdemir

Zeynep Özdemir
Inonu University · Department of Professional Pharmaceutical Sciences

PhD

About

39
Publications
28,263
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255
Citations
Citations since 2017
35 Research Items
247 Citations
2017201820192020202120222023020406080100
2017201820192020202120222023020406080100
2017201820192020202120222023020406080100
2017201820192020202120222023020406080100
Introduction
Pyridazinone derivatives, cholinesterase inhibitors, monoamine oxidase inhibitors

Publications

Publications (39)
Article
In this study, nine new benzothiazolone derivatives (6 a–i) were designed and synthesized to identify potent cholinesterase inhibitors. The compounds were tested in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and found to be selective to BChE. Compound 6 f proved the most potent derivative (IC50=12.25±0.23 μM) against...
Article
Human health and illness are dependent on lipases, which play a key role in maintaining cell integrity, storing fat for energy and serving as signaling molecules. In this study, 4 compounds that carry 6-phenylpyridazin-3(2H)-one main nucleus, which can be effective as lipase inhibitors, were synthesized and their structures were elucidated. The bio...
Article
Full-text available
Thirteen benzothiazolone derivatives (M1–M13) were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs) and monoamine oxidases (MAOs). All the compounds inhibited ChEs more effectively than MAOs. In addition, most of the compounds showed higher inhibitory activities against butyrylcholinesterase (BChE) than acetylc...
Article
Previously, some racemic 1-(phenyl/4-chlorophenyl)-2-(1H-triazole-1-yl)ethanol ester derivatives having a stereogenic center in their structure were synthesized and investigated for their anticonvulsant and antifungal activities. In this work, the direct enantiomeric separations of four compounds (1-4) were developed on the commercially available c...
Article
Full-text available
Sixteen compounds (TR1–TR16) were synthesized and evaluated for their inhibitory activities against monoamine oxidase A and B (MAOs). Most of the derivatives showed potent and highly selective MAO-B inhibition. Compound TR16 was the most potent inhibitor against MAO-B with an IC50 value of 0.17 μM, followed by TR2 (IC50 = 0.27 μM). TR2 and TR16 sel...
Article
Cholinesterase inhibition is of great importance in the fight against neurodegenerative disorders such as Alzheimer’s disease. Azole antifungals have come under the spotlight with recent discoveries that underline the efficacy and potential of miconazole and its derivatives against cholinesterase enzymes. In this study, we evaluated a library of az...
Article
Cancer, a disease defined by rapid proliferation of cells, still remains one of the most feared diseases of the modern world. Many structurally different anti-carcinogenic drugs are used in several tumor types such as bladder, colon, ovary, breast, head and neck, testis, lung and prostate cancer. In this study, cytotoxic effects of the compounds wi...
Article
In this study, 12 oxime derivatives were synthesized by using with conventional method and microwave irradiation method. It was aimed to compare the effectiveness of the conventional method and microwave method. Their yields were determined for both methods, and the yields increased when the microwave method was used. The compounds which have oxime...
Article
Depression is a serious psychological disorder that affects a significant population. We investigated the antidepressant activities of four pyridazinone derivatives that contain the hydrazide moiety using the forced swimming test (FST). The compounds tested exhibited good antidepressant activity compared to duloxetine. The most promising compound w...
Article
Azoles are first-line drugs used in fungal infections. Topical antifungals, such as miconazole and econazole, are known to be active against Gram-positive bacteria, which was reported to result from bacterial flavohemoglobin (flavoHb) inhibition. Dual antibacterial/antifungal action is believed to have benefits for antimicrobial chemotherapy. In th...
Article
Full-text available
Novel twenty−three 3(2H)−pyridazinone derivatives were designed and synthesized based on the chemical requirements related to the anti−proliferative effects previously demonstrated within this scaffold. The introduction of a piperazinyl linker between the pyridazinone nucleus and the additional (un)substituted phenyl group led to some compounds end...
Article
Background The MAO enzyme which is presented in the brain and peripheral tissues and is a significant enzyme that is responsible for the deamination of biogenic amines and thus regulation of neurotransmitter levels. The reaction of these neurotransmitters with MAO enzyme produces aldehyde and free amine. MAO enzyme consists of two isoforms, MAO-A a...
Article
Full-text available
Candida infections pose a serious public health threat due to increasing drug resistance. Azoles are first-line antifungal drugs for fungal infections. In this study, we tested an in-house azole collection incorporating naphthalene ring to find hits against planktonic and biofilm forms of resistant Candida spp. In the collection, potent derivatives...
Article
Full-text available
Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all compounds. Successive assays revea...
Article
Cancer is a disease caused by the disruption of the cell cycle, which is controlled by the cell's genetic material. Chemotherapy, radiotherapy and surgical methods are used as standard in cancer treatment. In chemotherapy, tumor cells are targeted to destroy or stop their growth. Due to the fact that the existing anticancer drugs do not have suffic...
Article
Full-text available
Twelve pyridazinones (T1-T12) containing the (2-fluorophenyl) piperazine moiety were designed, synthesized, and evaluated for monoamine oxidase (MAO)-A and-B inhibitory activities. T6 was found to be the most potent MAO-B inhibitor with an IC 50 value of 0.013 µM, followed by T3 (IC 50 = 0.039 µM). Inhibitory potency for MAO-B was more enhanced by...
Article
Full-text available
Azole antifungal drugs are commonly used in antifungal chemotherapy. Antibacterial effects of some topical antifungals, such as miconazole and econazole, have lately been revealed, which suggests a promising venue in antimicrobial chemotherapy. In this study, we tested an in‐house azole collection with antifungal properties for their antibacterial...
Article
Background Since brain neurotransmitter levels are associated with the pathology of various neurodegenerative diseases like Parkinson and Alzheimer, monoamineoxidase (MAO) plays a critical role in balancing these neurotransmitters in the brain. MAO isoforms appear as promising drug targets for the development of central nervous system agents. Pyrid...
Article
Full-text available
Abstract Aim: The aim of this study is to provide a qualitative and quantitative explanation of the structure activity relationships with pharmacophore analysis and Quantitative Structure Activity Relationship (QSAR) studies of the compounds synthesized as acetylcholinesterase enzyme inhibitor by our research group. Material and Methods: Maestro 11...
Article
Full-text available
Background Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh), which is a significant neurotransmitter for regulation of cognition in animals. Inhibition of cholinesterases is an effective method to curb Alzheimer’s disease, a progressive and fatal ne...
Article
Full-text available
Background: Butyrylcholinesterase (BChE) is known serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh). Although the role of the other serine hydrolase enzyme, acetylcholinesterase (AChE) in cholinergic transmission is well known, the role of BChE has not been elucidated sufficiently. The hydrolysis of acetylcholine in the...
Article
Systemic Candida infections pose a serious public health problem with high morbidity and mortality. C. albicans is the major pathogen identified in candidiasis, however non‐albicans Candida spp. with antifungal resistance are now more prevalent. Azoles are first‐choice antifungal drugs for candidiasis, however they are ineffective for certain infec...
Article
Background: The pyridazinone nucleus has been incorporated into a wide variety of therapeutically interesting molecules to transform them into better drugs. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known to be serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh). Inhibition of cholinesterases is an...
Article
Purpose: To synthesize a series of new 1-(2-naphthyl)-2-(1H-pyrazol-1-yl)ethanone oxime ester derivatives (5-12) with potential anticancer properties, and to determine their cytotoxic effects in mouse fibroblast and human neuroblastoma cell lines. Methods: The title compounds were obtained through sodium salt reaction of 1-(naphthalene-2-yl)-2(1H-...
Chapter
Alzheimer’s disease (AD) is a progressive and fatal neurodegenerative disease which deteriorates a person's ability to perform daily activities, leading to various neuropsychiatric symptoms and behavioral disorders in later stages of the disease. The pathophysiology of AD is complex. Biochemical studies indicate that some neuromediator levels, espe...
Article
In this study, seven new 3(2H)-pyridazinone derivatives expected to show cytotoxic activity in liver and colon cancer cell lines were synthesized. Their structures were confirmed by the IR, ¹H-NMR, ¹³C-NMR spectra and elementary analyses. Compunds V1-V7 were tested on HEP3B (liver cancer) and HTC116 (colon cancer) cell lines for cytotoxicity by usi...
Chapter
Full-text available
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh). Although the role of AChE in cholinergic transmission is well known, the role of BChE has not been elucidated sufficiently. The hydrolysis of acetylcholine in the synaptic healthy brain cells is main...
Article
Full-text available
A series of new ester derivatives were synthesized by the reaction of various acids with 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol and in vivo screened for their anticonvulsant activity. The title compounds were screened against MES and ScM seizure tests according to a modified version of the Epilepsy Therapy Screening Program (ETSP) p...
Article
Background: Brain cancer (neuroblastoma) and liver cancer (hepatocellular carcinoma) are common cancer types among others worldwide which do not have a radical treatment and cure. Objective: In the current study, five novel pyridazinone derivates bearing benzelhydrazone moiety at second position were synthesized and evaluated for their cytotoxic ac...
Article
The synthesis of ethyl 4-oxo-1,4-dihydroquinoline-3-carboxylates (4, 5) was performed via the reaction of corresponding anilines with diethyl ethoxymethylenemalonate under conventional and also microwave promoted conditions. The treatment of 4 and 5 afforded the corresponding hydrazides (6 and 7). These hydrazides were converted to the correspondin...
Article
Full-text available
Inhibition of cholinesterases is an effective method to curb Alzheimer’s disease, a progressive and fatal neurological disorder. A series of 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted benzalhidrazone) derivatives were designed, synthesized, and their inhibitory effects on acetylcholinesterase and butyrylcholinesterase were evaluated...
Article
In this study, 12 new oxime ether derivatives, which were expected to show anticonvulsant and antimicrobial activities, were synthesized. Oxime ether derivatives were synthesized by the reaction of various alkyl halides with 1-(2-naphthyl)-2-(pyrazol-1-yl)ethanone oxime. Anticonvulsant activity of the compounds was determined by maximal electroshoc...
Article
Full-text available
In present study a series of new 6-substituted-3(2H)-pyridazinone-2-acetyl-2- (substituted benzal) hydrazone derivatives were synthesized and evaluated for analgesic, and anti-inflammatory and antimicrobial activities. The structures of these new pyridazinone derivatives were confirmed by their IR, 1H-NMR spectra and elementary analysis. Analgesic...
Article
Full-text available
The title compound, 1-(naphthalene-2-yl)-2-(1H-pyrazol-1-yl)ethanone O-butyl oxime, I, was synthesized. The crystal and molecular structures of I were determined by IR, H-1-NMR, mass spectrum, elemental analysis and X-ray single crystal diffraction. Molecular geometry from X-ray experiment of I in the ground state was compared using the Density Fun...

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Project (1)
Project
Since the treatment approach with MAO-B inhibition has a place in the treatment of both Parkinson's and Alzheimer's disease, and AChE enzyme inhibition is of great importance in the treatment of Alzheimer's disease, it is aimed to carry out inhibition studies of both enzymes in vitro within the scope of this project. For this purpose, the synthesis of new compounds which were determined by molecular modeling studies and bound to the active sites of target enzymes at the highest level will be synthesized, and their structures will be elucidated. Then, in vitro inhibitory activities of the compounds on the targeted enzymes will be determined.