Araştırmacılar Yahya Nural
Yahya NuralECZACILIK FAKÜLTESİ TEMEL ECZACILIK BİLİMLERİ BÖLÜMÜ ANALİTİK KİMYA ANABİLİM DALI
169602

Is anti-IgE therapy effective in preventing magnesium and selenium loss in bones of mice with chronic allergic asthma?

Nural, Yahya | Erdal, Nurten | Uzun, Coşar

Objective: Chronic allergic asthma (CA) is a respiratory disease that affects millions of people worldwide. While there is evidence linking airway hyperresponsiveness and asthma to factors related to bone metabolism, the impact of asthma on bone health is not well understood. Therefore, to explore whether: (i) CA causes meaningful changes in bone magnesium (Mg) and selenium (Se) levels, and if any, (ii) anti-IgE (anti-immunoglobulin E) treatment has a protective effect against these changes. Methods: In present study used tibia bones from a previous study on CA in mice. A murine model was used to generate CA. Thirty-two BALB/c male mice were randomly divided into four equal sized groups (eight mice/group): control group (intact), CA (treated with saline (0.9% NaCl), CA+L-AIgE (100 μg of a...

Makale2023Dicle Medical Journal 2 | 0 Erişime Açık
169301

New naphthoquinone thiazole hybrids as carbonic anhydrase and cholinesterase inhibitors: Synthesis, crystal structure, molecular docking, and acid dissociation constant

Efeoglu, Cagla | Selcuk, Ozge | Demir, Bunyamin | Nural, Yahya

In this study, N-[3-(3-amino-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-R-thiazol-2(3H)-ylidene]-2,6-difluorobenzamide derivatives as new 1,4-naphthoquinone thiazole hybrids were synthesized by reacting of N-[(3amino-1,4-dioxo-1,4-dihydronaphthalen-2-yl)carbamothioyl]-2,6-difluorobenzamide with various alpha-bromoketones in 76-92% yields. Their molecular structures were characterized by 1H NMR, 13C NMR, 19F NMR, FT-IR, and HRMS, and the stereochemistry of one of the hybrids was determined by single crystal x-ray diffraction study. These synthesized new compounds (3a-e) were found to be effective inhibitor molecules for cholinesterases (butyrylcholinesterase (BChE) and acetylcholinesterase (AChE)), and carbonic anhydrase I and II (hCA I and hCA II) enzymes. KI values were found to be in the ra...

169442

Synthesis, antimicrobial activity and acid dissociation constants of methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives

Nural, Yahya | Gemili, Muge | Ulger, Mahmut

In this study, a series of polysubstituted methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives were designed and synthesized by the cyclization reaction of methyl 1-(benzoylcarbamothioyl)-5,5-diphenylpyrrolidine-2-carboxylates and 2-bromo-1-(4-substituted phenyl) ethanones in 70-96% yield. The starting pyrrolidine derivatives were synthesized via a 1,3-dipolar cycloaddition reaction in 83-88% yield. The stereochemistry of one of these methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives was characterized by a single crystal X-ray diffraction study and the acid dissociation constants of these compounds were determined. An antimicrobial screening was performed against different bacterial and fungal strains and against the M. tuberculosis H37Rv strai...

169444

Novel 1,4-naphthoquinone N-aroylthioureas: Syntheses, crystal structure, anion recognition properties, DFT studies and determination of acid dissociation constants

Gemili, Müge | Nural, Yahya

In this paper, five novel 1,4-naphthoquinone N-aroylthiourea derivatives were synthesized, by the reaction of 2,3-diaminonaphthalene-1,4-dione and aroylisothiocyanates, in excellent yield (88-96%) and characterized by using FT-IR, H-1/C-13 NMR and HRMS. In addition, the molecular structure of one of the 1,4-naphthoquinone N-aroylthiourea compounds was characterized by single crystal X-ray diffraction studies. The absorption spectra of the compounds were determined in DMSO and the dyes have absorption in visible region in the range of 464-477 nm. The chemosensing ability of each of the prepared dyes was assessed by titrating them towards the anions; F-, Cl-, Br-, I- AcO-, CN-, CIO4-, H2PO4-, HSO4-, and NO3-, using spectrophotometric and H-1 NMR titration techniques in DMSO, experimentally. ...

169445

Synthesis, Biological Evaluation, Molecular Docking, and Acid Dissociation Constant of New Bis-1,2,3-triazole Compounds

Nural, Yahya | Ozdemir, Sadin | Yalcin, Mustafa Serkan | Demir, Bunyamin

In this study, new bis-1,2,3-triazole derivatives, N,N '-(1,3-phenylene)bis(2-(4-R-1H-1,2,3-triazol-1-yl)acetamide), were synthesized by copper-catalyzed azide-alkyne cycloaddition click chemistry in 84-96 % yield. A wide range bioactivity screening was performed to determine DNA cleavage, antioxidant, antibacterial and antifungal activities. All of the synthesized bis-1,2,3-triazoles showed excellent DNA cleavage activity and 4 e, bearing 2-bromoethyl moiety as a substituent, was almost degraded all of the plasmid DNA. Molecular docking simulations suggest that the synthesized compounds act as minor groove binders of DNA. The antioxidant activities of the bis-1,2,3-triazoles were determined based on the radical scavenging effect of the stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) free...

169456

Synthesis, antimycobacterial activity, and acid dissociation constants of polyfunctionalized 3-[2-(pyrrolidin-1-yl)thiazole-5-carbonyl]-2H-chromen-2-one derivatives

Nural, Yahya

This study reports on synthesis and determination of antimycobacterial activity and acid dissociation constants of polyfunctionalized 3-[2-(pyrrolidin-l-yl)thiazole-5-carbonyl[-2H-chromen-2-one derivatives, containing thiazole, coumarin, and pyrrolidine octahydropyrrolo[3,4-c]pyrrole moieties. The products were synthesized by a cyclization reaction of 5,5-diphenylpyrrolidine N-aroylthioureas or methyl 5-substituted 4,6-dioxo-3,3-diphenyloctahydropyrrolo[3,4-c[pyrrole-lcarboxylate N-aroylthioureas and 3-(bromoacetyl)coumarin with good to excellent yield (81-97%). The compounds exhibited antimycobacterial activity against the M. tuberculosis H37Rv strain with minimum inhibitory concentration values in the range of 31.25-125 mu g/cm(3). Acid dissociation constants of the compounds were determ...

169458

Synthesis, crystal structure, DFT studies, acid dissociation constant, and antimicrobial activity of methyl 2-(4-chlorophenyl)-7a-((4-chlorophenyl)carbamothioyl)-1-oxo-5,5-diphenyl-3-thioxo-hexahydro-1H-pyrrolo[1,2-e]imidazole-6-carboxylate

Nural, Yahya | Gemili, Muge | Ulger, Mahmut

A novel bicyclic thiohydantoin fused to pyrrolidine compound, methyl 2-(4-chlorophenyl)-7a-((4-chlorophenyl)carbamothioyl)-1-oxo-5,5-diphenyl-3-thioxo-hexahydro-1H-pyrrolo[1,2-e]imidazole-6-carboxylate, was synthesized by the cyclization reaction of dimethyl 5,5-diphenylpyrrolidine-2,4-dicarboxylate and 4-chlorophenyl isothiocyanate in the presence of 4-(dimethylamino)pyridine to form methyl 2-(4-chlorophenyl)-1-oxo-5,5-diphenyl-3-thioxo-hexahydro-1H-pyrrolo[1,2-e]imidazole-6-carboxylate with concomitant addition reaction of the 4-chlorophenyl isothiocyanate in 79% yield. The structural characterization was performed by NMR, FT-IR, MS and HRMS techniques, and the stereochemistry of the compound was determined by single crystal X-ray diffraction study. In addition, the molecular structure a...

169459

A Review on the Design, Synthesis, and Structure-activity Relationships of Benzothiazole Derivatives against Hypoxic Tumors

Nural, Yahya | Ayaz, Furkan

There has been a growing body of studies on benzothiazoles and benzothiazole derivatives as strong and effective anti-tumor agents against lung, liver, pancreas, breast, and brain tumors. Due to the highly proliferative nature of the tumor cells, the oxygen levels get lower than that of normal tissues in the tumor microenvironment. This situation is called hypoxia and has been associated with increased ability for carcinogenesis. For the drug design and development strategies, the hypoxic nature of the tumor tissues has been exploited more aggressively. Hypoxia itself acts as a signal initiating system to activate the pathways that eventually lead to the spread of the tumor cells into the different tissues, increases the rate of DNA damage, and eventually ends up with more mutation levels ...

169461

Synthesis of novel immunomodulatory 1,4-disubstituted bis-1,2,3-triazoles by using click chemistry and their intracellular mechanism of action

Nural, Yahya | Acar, Irem | Yetkin, Derya | Efeoglu, Cagla | Ayaz, Furkan

In this study, six new 1,4-disubstituted bis-1,2,3-triazole compounds, N,N '-(1,2-phenylene)bis(2-(4-R-1H-1,2,3triazol-1-yl)acetamide), were synthesized with high yield (88-96 %) by using click chemistry and their molecular structures were characterized by using NMR, FT-IR, HRMS and elemental analysis techniques. Previous studies suggest anti-inflammatory and analgesic activities for different 1,2,3-triazole derivatives and in the light of those studies we aimed to examine these novel derivatives immunomodulatory activities on the mammalian macrophages. Pro-inflammatory cytokines (TNF, IL6, GMCSF and IL12p40) secretion levels were tested in the presence of bis-1,2,3-triazole compounds when the macrophages were activated with LPS. These new derivatives were able to suppress the product...

169473

Does anti-IgE therapy prevent chronic allergic asthma-related bone deterioration in asthmatic mice?

Nural, Yahya

Current evidence on the association between allergic diseases and bone metabolism indicates asthma may be a potential risk factor for bone health. Using anti-IgE has been proven effective in allergic asthma treatment with a good safety profile; however, its effects on bone health are unknown. Thus, we aimed to investigate whether: (i) chronic allergic asthma (CAA) causes any meaningful changes in bone, and if any, (ii) anti-IgE therapy prevents any CAA-induced adverse alteration. A murine model was used to study CAA. Thirty-two BALB/c male-mice were assigned into four groups (eight-mice/group): Control, CAA (treated with saline), CAA + 100 mu g of anti-IgE (CAA + 100AIgE), and CAA + 200 mu g of anti-IgE (CAA + 200AIgE) groups. After immunization, saline or anti-IgE was performed intraperit...

169317

Novel highly functionalized 1,4-naphthoquinone 2-iminothiazole hybrids: Synthesis, photophysical properties, crystal structure, DFT studies, and anti(myco)bacterial/antifungal activity

Gemili, Muge | Nural, Yahya | Ülger, Mahmut | Erat, Selma

In this paper, a series of novel highly functionalized 1,4-naphthoquinone 2-iminothiazole hybrids were synthesized via a cyclization reaction of 2,3-diaminonaphthalene-1,4-dione N-aroylthioureas and alpha-bromoketones in good to excellent yields (74-94%). The stereochemistry of one of the 1,4-naphthoquinone 2-iminothiazole products was characterized by single crystal X-ray diffraction technique. Photophysical properties of the compounds in DMSO, HAc and THF were determined by using UV-vis spectroscopy. The ground state geometries and the absorption spectra of the compounds were also determined using Density Functional Theory (DFT) and time-dependent DFT (TD-DFT) at B3LYP/631 + g(d,p) level of theory. The computed results are consistent with experimental values. An antimicrobial screening w...

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