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Chinese Journal of Chemistry 2018年第9期36卷 837-844页

作者： Murat Kaloglu Nazan Kaloglur ismail ozdemir Department of Chemistry Faculty of Science and Arts inonu University 44280 Malatya Turkey Catalysis Research and Application Center inonu University 44280Malatya Turkey

Herein, we report that a series of novel palladium（II）-NHC complexes （NHC=N-heterocyclic carbene） were synthesized. The structures of all novel complexes were characterized by ^1H NMR, ^13C NMR, FT-IR spectroscopy and elemental analysis techniques. These palladium（ll）-NHC complexes were tested as efficient catalysts in the direct C-H bond activation of benzoxazole and benzothiazole with aryl bromides in the presence of 1 mol% catalyst loading at 150 ℃ for 4 h. Under the given conditions, various aryl bromides were successfully applied as the arylating reagents to achieve the 2-arylbenzoxazoles and 2-arylbenzothiazoles in acceptable to high yields.

关键词： benzimidazolium bromide benzoazoles direct C-H bond activation N-heterocyclic carbene palladium

The effect of α-blocker therapy on erectile functions in patients with lower urinary tract symptoms due to benign prostate hyperplasia

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Asian Journal of Andrology 2009年第6期11卷 716-722页

作者： Omer Demir ismail ozdemir Ozan Bozkurt Guven Asian Ahmet Adil Esen Dokuz Eylul University Medical School Department of Urology Inciralti Izmir 35340 Turkey

In this study we aimed to evaluate the impact of doxazosin treatment on erectile functions in patients with lower urinary tract symptoms （LUTS） and having erectile dysfunction （ED） at baseline. Fifty-three patients with LUTS （IPSS score 〉 7） whose maximum flow rate （Qmax）〈 15 mL s-1 and PSA 〈 4 ng dL^-1 were enrolled in the study. Patients received doxazosin 4 nag once daily for 6 weeks. Subjective efficacy was assessed by IPSS, IPSS- Quality of Life （IPSS-QoL） for LUTS and efficacy was assessed by International Index of Erectile Function （IIEF） for erectile functions at baseline and sixth weeks. The objective efficacy was assessed by Q The patients were classified according to their self reported erectile status： group I had ED and group II did not have ED. At the endpoint, doxazosin significantly improved the total IPSS score （-7.7 ±6.1, P = 0.006）, IPSS-QoL score （-1.5 ± 1.5, P = 0.024） and Qmax （3.2 ± 4.6 mL s^-1, P = 0.002） over baseline. Mean decrease in IPSS and IPSS-QoL scores after the treatment period were 6.9 ＋ 6.4 （P 〈 0.001） and 0.95 4- 1.80 （P 〈 0.05） in group I, whereas 8.2 4- 5.8 （P 〈 0.001） and 1.9 4- 1.1 in group IX （P 〈 0.001）, respectively. Mean changes of Qmax values were 2.3 4- 3.3 mL s^-1 in group I （P 〈 0.05） and 3.7 4- 5.3 mL s-1 in group II （P 〈 0.001）. The improvement of IIEF-EF scores after the treatment period was only significant for group I. The efficacy of a-blocker therapy for LUTS was better by means of symptomatic relief for patients who did not have ED when compared with patients who had ED at baseline. However, slight improvement in erectile functions with a-blocker therapy was only seen in LUTS patients with ED.

关键词： benign prostate hyperplasia doxazosinlerectile dysfunction lower urinary tract symptoms treatment outcome

Possible Mechanism of Action of Neurokinin-1 Receptors （NK1R） Antagonists

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Journal of Pharmacy and Pharmacology 2017年第11期5卷 787-797页

作者： Ozum Ozturk Esin Aki-Yalcin Tugba Ertan-Bolelli Kayhan Bolelli Andry Nur-Hidayat Ozlem Bingol-Ozakpinar Filiz ozdemir ismail Yalcin Pharmacy Chemistry Department Faculty of Pharmacy Ankara University Ankara 06100 Turkey Bioinformatics Department Biotechnology Institution Ankara University Ankara 06100 Turkey Biochemistry Department Faculty of Pharmacy Marmara University Istanbu134722 Turkey Analytical Chemistry Department Faculty of Pharmacy Marmara University Istanbu134722 Turkey

Recently, NK1R （Neurokinin-1 receptors） take attention as new and promising target in anticancer drug development area. It has been proved that non-peptide NK1R antagonists L-733,060, aprepitant and L-732,138 inhibited tumor growth in several cancer cell lines. For the development of novel NK1R antagonists as antitumor agents, heterocyclic compounds which were previously synthesized by our team, tested for their cytotoxic activities in several cancer cell lines in this study. Among the tested compounds, a benzothiazole derivative BSN-009 inhibited colon cancer cell lines growth by 57.53% by comparing the activity to the control drug aprepitant. Molecular modeling studies such as molecular docking and pharmacophore generation were performed with known NK1R antagonists and BSN-009 by using Discovery Studio 3.5 in order to explain their binding modes to NK1R. BSN-009 may be a good anticancer drug candidate as a possible NK1R antagonist and is worthy to carry on the anticancer studies.

关键词： Anticancer aprepitant benzothiazole docking NK1 receptor antagonist pharmacophore.

Combined metabolic activators improve cognitive functions in Alzheimer’s disease patients:a randomised,double-blinded,placebo-controlled phase-II trial

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Translational Neurodegeneration 2023年第1期12卷 849-871页

作者： Burak Yulug Ozlem Altay Xiangyu Li Lutfu Hanoglu Seyda Cankaya Simon Lam Halil Aziz Velioglu Hong Yang Ebru Coskun Ezgi Idil Rahim Nogaylar Ahmet Ozsimsek Cemil Bayram ismail Bolat Sena Oner Ozlem ozdemir Tozlu Mehmet Enes Arslan Ahmet Hacimuftuoglu Serkan Yildirim Muhammad Arif Saeed Shoaie Cheng Zhang Jens Nielsen Hasan Turkez Jan Borén Mathias Uhlén Adil Mardinoglu Department of Neurology and Neuroscience Faculty of MedicineAlanya Alaaddin Keykubat UniversityAntalyaTurkey Science for Life Laboratory KTH-Royal Institute of TechnologyStockholmSweden Department of Neurology Faculty of MedicineIstanbul Medipol UniversityIstanbulTurkey Centre for Host-Microbiome Interaction’s Faculty of DentistryOral and Craniofacial SciencesKing’s College LondonLondonUK Department of Women’s and Children’s Health Karolinska InstituteStockholmSweden Functional Imaging and Cognitive-Affective Neuroscience Lab Istanbul Medipol Univer-sityIstanbulTurkey Department of Medical Pharmacology Faculty of Medi-cineAtatürk UniversityErzurumTurkey Department of Pathology Veterinary FacultyAtaturk UniversityErzurumTurkey Department of Molecular Biology and Genetics Faculty of ScienceErzurum Technical UniversityErzurumTur-key School of Pharmaceutical Sciences Zhengzhou UniversityZhengzhouPeople’s Republic of China Department of Biology and Biological Engineering Chalmers University of TechnologyGothenburgSweden Department of Medical Biology Faculty of MedicineAtatürk UniversityErzurumTurkey Department of Molecular and Clinical Medicine University of Gothenburg and Sahlgrenska University HospitalGothenburgSweden.

Background Alzheimer’s disease(AD)is associated with metabolic abnormalities linked to critical elements of *** recently administered combined metabolic activators(CMA)to the AD rat model and observed that CMA improves the AD-associated histological parameters in the *** promotes mitochondrial fatty acid uptake from the cytosol,facilitates fatty acid oxidation in the mitochondria,and alleviates oxidative *** Here,we designed a randomised,double-blinded,placebo-controlled phase-II clinical trial and studied the effect of CMA administration on the global metabolism of AD ***-dose CMA included 12.35 g L-serine(61.75%),1 g nicotinamide riboside(5%),2.55 g N-acetyl-L-cysteine(12.75%),and 3.73 g L-carnitine tartrate(18.65%).AD patients received one dose of CMA or placebo daily during the first 28 days and twice daily between day 28 and day *** primary endpoint was the difference in the cognitive function and daily living activity scores between the placebo and the treatment *** secondary aim of this study was to evaluate the safety and tolerability of CMA.A comprehensive plasma metabolome and proteome analysis was also performed to evaluate the efficacy of the CMA in AD *** We showed a significant decrease of AD Assessment Scale-cognitive subscale(ADAS-Cog)score on day 84 vs day 0(P=0.00001,29%improvement)in the CMA ***,there was a significant decline(P=0.0073)in ADAS-Cog scores(improvement of cognitive functions)in the CMA compared to the placebo group in patients with higher ADAS-Cog *** cognitive functions in AD patients were supported by the relevant alterations in the hippocampal volumes and cortical thickness based on imaging ***,the plasma levels of proteins and metabolites associated with NAD+and glutathione metabolism were significantly improved after CMA *** Our results indicate that treatment of AD patients with CMA can lead to enhanced cognit

关键词： Alzheimer’s disease Combined metabolic activators Multi-omics Systems biology Systems medicine