A5041891392- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Quinazolinone synthesis and applications
- Multicomponent Synthesis of Heterocycles
- Synthesis and Biological Evaluation
- Phenothiazines and Benzothiazines Synthesis and Activities
- Computational Drug Discovery Methods
- Analytical Chemistry and Chromatography
- Microfluidic and Capillary Electrophoresis Applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Cancer therapeutics and mechanisms
- Antifungal resistance and susceptibility
- Microbial Natural Products and Biosynthesis
- Bioactive Compounds and Antitumor Agents
- Pharmaceutical studies and practices
- Synthesis of heterocyclic compounds
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Fungal Plant Pathogen Control
- Innovative Microfluidic and Catalytic Techniques Innovation
- Chromatography in Natural Products
- Molecular spectroscopy and chirality
- Medical Education and Admissions
- Synthesis and Reactivity of Heterocycles
- Natural Antidiabetic Agents Studies
Hacettepe University
2007-2024
Başkent University
2024
Manisa Celal Bayar University
2019
4-Aryl-7,7-dimethyl-5-oxo-1,2,3,4,5,6,7,8-octahydroquinazoline-2-thione derivatives (1-8) have been prepared by modified Biginelli reaction from 5,5-dimethyl-1,3-cyclohexanedione, the aromatic aldehydes and thiourea. The structures of compounds were confirmed spectroscopic elemental analysis. Racemic resolved into their enantiomers HPLC using an amylose tris-(3,5-dimethylphenylcarbamate) chiral stationary phase in normal mode. calcium antagonist activities determined tests performed on...
(Arylalkyl)azoles are a class of antiepileptic compounds including nafimidone, denzimol, and loreclezole (LRZ). Nafimidone denzimol thought to inhibit voltage‐gated sodium channels (VGSCs) enhance γ‐aminobutyric acid (GABA)‐mediated response. LRZ, positive allosteric modulator A‐type GABA receptors (GABA A Rs), was reported be sensitive Asn265 the β2/β3 subunit. Here, we report new N ‐[1‐(4‐chlorophenyl)‐2‐(1 H ‐imidazol‐1‐yl)ethylidene]hydroxylamine esters showing anticonvulsant activity in...
Diabetes mellitus, a chronic disorder characterized by hyperglycemia, is considered pandemic of modern times. α-Glucosidase inhibitors emerged as promising class antidiabetic drugs with better tolerability compared its alternatives. Azoles, although widely preferred in drug design, have scarcely been investigated for their potential against α-glucosidase. In this study, we evaluated α-glucosidase inhibitory effects 20 azole derivatives selected out an in-house collection via structure-based...
Abstract Azole antifungal drugs are commonly used in chemotherapy. Antibacterial effects of some topical antifungals, such as miconazole and econazole, have lately been revealed, which suggests a promising venue antimicrobial In this study, we tested an in‐house azole collection with properties for their antibacterial activity to identify dual‐acting hits using the broth microdilution method. The vitro screen yielded number potent derivatives against gram‐positive bacteria, Enterococcus...
Abstract Fungal infections have become a major public health issue with dramatically increasing morbidity, mortality and cost of hospitalization. Azole antifungals are first‐in‐line medications against most types mycoses azoles having an oxime moiety, although not extensively investigated, were reported to great antifungal potential, as well as, activity Gram‐positive bacteria. In the current study, new series 2‐(1 H ‐imidazol‐1‐yl)‐1‐phenylethanone esters ( 5 – l ) synthesized tested for...
In this study, the synthesis of some new 2-thioxo-1,2,3,4-tetrahydropyrimidines and their condensed derivatives, thiazolo[3,2-α] pyrimidines, are described. The structures compounds were confirmed by IR, 1H-NMR, 13C-NMR, mass spectroscopy. direct high-performance liquid chromatographic separation on derivatized cellulose chiral stationary phases such as tris(3,5-dimethylphenylcarbamate) (OD), tris(4-methylphenylcarbamate) (OG), tris(4-methylbenzoate) (OJ) was studied. All screened for...
Abstract A series of 1,2,3,4‐tetrahydro‐6‐methyl‐4‐(substituted phenyl)‐2‐thioxo‐5‐pyrimidinecarboxylic acid methyl esters were synthesized by condensing thiourea with acetoacetate and nonsubstituted or differently substituted benzaldehydes in absol. ethanol using HCl as a catalyst according to the Biginelli reaction. The structures compounds confirmed elemental spectroscopic analysis. ‐ evaluated for their calcium antagonistic activity on basis potency inhibiting [ 3 H] PN 200—110 binding...
Abstract 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‐ spp. antifungal resistance are now more prevalent. Azoles first‐choice drugs for they ineffective certain caused by resistant strains. block ergosterol synthesis inhibiting fungal CYP 51, which leads to disruption of membrane permeability. In this study, we screened activity an in‐house azole library 65...
Abstract Eleven new 7‐[2‐(dihydro‐5‐substituted‐6‐thioxo‐2 H ‐1,3,5‐thiadiazine‐3(4 )‐yl)‐2‐(4‐hydroxyphenyl)acetamido]‐3‐methyl‐3‐cephem‐4‐carboxylic acid derivatives were synthesized by the reaction of cefadroxil monohydrate, formaldehyde and substituted potassium dithiocarbamate. Their structures have been elucidated spectral data elementary analysis. The title compounds tested for antimicrobial activity in vitro against gram‐positive bacteria ( Staphylococcus aureus, Streptococcus...
Background/Objectives: The increase in fungal infections, both systemic and invasive, is a major source of morbidity mortality, particularly among immunocompromised people such as cancer patients organ transplant recipients. Because their strong therapeutic activity excellent safety profiles, azole antifungals are currently the most extensively used antifungal drugs. Antibacterial properties various topical antifungals, oxiconazole, which features oxime ether functionality, were discovered,...
6-Ethyl-4-aryl-5-methoxycarbonyl-3,4-dihydropyrimidin-2(1H)-one derivatives (1-10) were synthesized by condensing urea with methyl 3-oxopentanoate and aromatic aldehydes in absol. ethanol using HCl as a catalyst according to the Biginelli reaction. The structures of compounds confirmed spectroscopic elemental analysis. calcium channel blocker activities determined tests performed on isolated rat ileum lamb carotid artery. On ileum, compound 2 was found be more effective at 10(-5) mol/L...
ABSTRACT Racemic 4-aryl-1,2,3,4,5,6,7,8-octahydroquinazoline-2-thiones were resolved into their enantiomers by HPLC on cellulose tris(4-methylbenzoate) coated silica gel using ethanol:n-hexane (70:30) as a mobile phase. A convenient method for preparation of chiral stationary phase was described and the characterized some chromatographic data.