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    Amelioration potential of synthetic oxime chemical cores against multiple sclerosis and Alzheimer's diseases: Evaluation in aspects of in silico and in vitro experiments
    (Elsevier B.V., 2024) Yılmaz, Anıl; Koca, Murat; Ercan, Selami; Acar, Özden Özgün; Boğa, Mehmet; Şen, Alaattin; Kurt, Adnan
    Alzheimer disease (AD) and multiple sclerosis (MS) are inflammatory neurological disorders. The main symptom of AD is dementia, and the main symptoms of MS are vertigo, sexual dysfunction, cognitive problems, and fatigue. Today, millions of people are affected by AD and MS, and the number is growing day by day. However, there are not any accurate remedies for both disorders. For this reason, discovering novel drug molecules against neurological disorders such as AD and MS is essential and precious. Oximes and benzofurans exhibit many pharmacological effects including anti-inflammatory and neurological activities. Thus, several novel compounds bearing oxime and benzofuran chemical cores were designed and synthesized, and their in vitro anticholinesterase activities were investigated in our previous study. A number of the synthesized molecules showed excellent anticholinesterase activity against both AChE and BChE enzymes. The mentioned study constituted a background for this study. In this study, we picked different chemical skeletons among all the synthesized molecules to conduct further in silico and in vitro experiments. In order to support our in vitro anticholinesterase findings, we also examined in silico anti-Alzheimer activity of the selected molecules. In addition, in silico and in vitro activities against MS disease of the synthesized molecules were investigated. Molecule 4 extraordinarily showed outstanding activity against AD disease both in silico and in vitro, as well as in silico activity against MS disease. This feature makes molecule 4 a possible drug lead molecule which is very limited in the market. On the other hand, molecule 1, a less substituted oxime skeleton, demonstrated the strongest in vitro activity against MS disease through in vitro anti-inflammatory effect. As an observation, molecule 4 was determined to be the most promising molecule to focus on in the further steps.
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    Synthesis of novel oxime and benzofuran chemical frameworks possessing potent anticholinesterase activity: A SAR study related to alzheimer disease
    (John Wiley and Sons Inc., 2023) Yılmaz, Anıl; Koca, Murat; Boğa, Mehmet; Kurt, Adnan; Öztürk, Turan
    Alzheimer Disease (AD) is a neurological disorder that causes the brain to shrink and brain cells to eventually die. Main symptom of AD is dementia. Today, approximately 50 million people worldwide are estimated to have AD. However, there is not a determined cure known against AD today. There are just four drugs against AD on the market. Unfortunately, none of them can totally destroy AD. Thus, discovering new molecules having capability to treat AD is required and significant. Benzofurans and oximes demonstrate a number of biological effects including anti-inflammatory and brain-barrier penetrating. For this reason, a number of novel compounds bearing oxime and benzofuran skeletons were designed and synthesized, and their anticholinesterase activities were investigated. Based on the results, several molecules demonstrated very strong anticholinesterase activities against both AChE and BChE enzymes, even much better than the reference drug molecule, Galantamine. Besides, structure-activity relationship (SAR) studies belonging to these chemical cores were revealed through this study for the first time. Various derivatives with different types of selective activities were obtained, which brightens the detailed SAR tendency of these molecules. This study can contribute to discover a novel lead drug molecule against AD, which is an urgent need.