A5042651919- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Computational Drug Discovery Methods
- Synthesis and Biological Evaluation
- Click Chemistry and Applications
- Inflammatory mediators and NSAID effects
- Cancer therapeutics and mechanisms
- Tuberculosis Research and Epidemiology
- Phenothiazines and Benzothiazines Synthesis and Activities
- Alzheimer's disease research and treatments
- Synthesis and Characterization of Heterocyclic Compounds
- melanin and skin pigmentation
- Synthesis of β-Lactam Compounds
- Multicomponent Synthesis of Heterocycles
- X-ray Diffraction in Crystallography
- Synthesis and Reactions of Organic Compounds
- Crystallization and Solubility Studies
- Synthesis and Reactivity of Heterocycles
- Biochemical Analysis and Sensing Techniques
- Nicotinic Acetylcholine Receptors Study
- Chemical Synthesis and Analysis
- Endodontics and Root Canal Treatments
- Skin Protection and Aging
- Phosphodiesterase function and regulation
- Phytochemicals and Antioxidant Activities
Hacettepe University
2014-2024
Birla Institute of Technology and Science, Pilani
2022
Ankara (Czechia)
2015
University of Calgary
2010
A series of synthetic chalcones and pyrazoline derivatives showed antityrosinase, anticancer considerable tubulin polymerization activity.
Hyperpigmentation in human skin and enzymatic browning fruits, which are caused by tyrosinase enzyme, not desirable. Investigations the discovery of enzyme inhibitors search for improved cytotoxic agents continue to be an important line drug development. In present work, a new series 30 compounds bearing α,β-unsaturated carbonyl moiety was designed synthesized following curcumin as model. All were evaluated their effects on cancer cell lines mushroom enzyme. Moreover, structure-activity...
In order to find novel cyclooxygenase (COX)‐2 inhibitors for treating inflammatory‐based diseases such as Alzheimer's disease (AD), an ethyl carboxylate side chain was added 5‐(4‐chlorophenyl)‐6‐(4‐(methylsulfonyl)phenyl)‐3‐(methylthio)‐1,2,4‐triazine (lead compound II ) maintain residual inhibition of COX‐1 through interacting with Arg120. A preliminary molecular docking study on both the COX‐1/COX‐2 active sites truly confirmed our hypothesis. Accordingly, a series...
To find out new agents for treating inflammatory-involved diseases such as Alzheimer's disease, a series of 1,2-diaryl-2-hydroxyiminoethanones containing vicinal diaryl pharmacophore COX inhibitors were tested by set in vitro, vivo, and computational studies. The vivo study compounds indicated their prominent anti-inflammatory ability at the doses 10 20 mg/kg comparable to celecoxib (10 mg/kg). Further vitro COX-1/COX-2 evaluations revealed that 4-methoxy derivative 3 had high selective...
A novel series of 2-pyrazoline derivatives were designed, synthesized, and evaluated for cholinesterase (ChE) inhibitory, Aβ anti-aggregating neuroprotective activities. Among these, 3d, 3e, 3g, 3h established as the most potent selective BChE inhibitors (IC50 = 0.5-3.9 μM), while 3f presented dual inhibitory activity against AChE 6.0 6.5 μM, respectively). Kinetic analyses revealed that 3g is a partial noncompetitive inhibitor (Ki 2.22 exerts competitive inhibition on 0.63 μM). The active...
This study reports the synthesis and evaluation of a series new pyridazin-3-ones with furan moieties 5a-j 6a-f, to test for their antimycobacterial antifungal activities. The structures target compounds were confirmed by elemental analysis spectroscopic techniques (IR, mass, 1H- 13C- NMR). Amongst tested, 5e, 5g, 5i 6e exhibited highest activity against Mycobacterium tuberculosis, while 5h, 6d 6f showed moderate in vitro activities C. albicans parapsilosis.
Some isoxazolo[4,5-d]pyridazin4(5H)-one derivatives were synthesized and tested for their analgesic activity. The activities of the compounds determined by hot-plate acetic acid writhing tests using morphine diclofenac as references. Compounds 4a, 4f, 4g, 4i (25 mg/kg) showed profiles similar to that (5 mg/kg).
Sixteen 3-aryl-5-(4-fluorophenyl)-N-substituted-4,5-dihydro-1H-pyrazole-1-carbothioamide derivatives were synthesized and their structure identified by UV, IR, (1) H NMR, mass spectra, microanalyses. The compounds evaluated in vitro for human monoamine oxidase (hMAO) inhibitory activities MAO-A -B selectivity. All the found to potently inhibit isoforms. 5-(4-Fluorophenyl)-3-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide (1.0 × 10(-3) µM) was hMAO-A most selectively...
The aim of this study was to synthesize, characterize, and screen some new 1-(4-((2-(4-substitutedphenyl)hydrazono)methyl)phenyl)-1H-1,2,4-triazole derivatives for their antimycobacterial activities.The target compounds (2a-h) were gained by condensation 4-(1H-1,2,4-triazol-1-yl)benzaldehyde with appropriate phenylhydrazines. Their structures elucidated IR, 1H-NMR, mass spectrometry. activities the determined in vitro against Mycobacterium tuberculosis H37Rv.The biological assay results...
This study evaluated monomer release and cytotoxicity of different adhesive restoration materials used for dental restorations. The extracts (1, 2, 7 days) three types materials, [Quixfill (QF), Silorane Restorative (SR), Ketac N 100 (KR)], the resins, [XP Bond (XP), Primer (SP), (KP), (SB)] were analyzed using high performance liquid chromatography/mass spectrometry (HPLC-MS). levels determined at time points (24, 48, 72 h) cell culture 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H...