A5050430964- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Synthesis and Characterization of Heterocyclic Compounds
- Click Chemistry and Applications
- Multicomponent Synthesis of Heterocycles
- Computational Drug Discovery Methods
- Synthesis of heterocyclic compounds
- Quinazolinone synthesis and applications
- Analytical Chemistry and Chromatography
- Synthesis and Reactions of Organic Compounds
- Essential Oils and Antimicrobial Activity
- Phytochemistry and Biological Activities
- Phytochemicals and Antioxidant Activities
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Synthesis of Organic Compounds
- Free Radicals and Antioxidants
- Fungal Plant Pathogen Control
- Natural product bioactivities and synthesis
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Adipokines, Inflammation, and Metabolic Diseases
- Eicosanoids and Hypertension Pharmacology
- Phytochemical compounds biological activities
- Melanoma and MAPK Pathways
- Heme Oxygenase-1 and Carbon Monoxide
- Nigella sativa pharmacological applications
Iuliu Hațieganu University of Medicine and Pharmacy
2016-2025
Yahoo (United Kingdom)
2015
Antimicrobial resistance is an increasing problem for global public health. One of the strategies to combat this issue synthesis novel antimicrobials through rational drug design based on extensive structure–activity relationship studies. The thiazole nucleus a prominent feature in structure many authorized antimicrobials, being clubbed with different heterocycles. purpose review study antimicrobial thiazoles various heterocycles, as reported literature between 2017 and 2023, order offer...
The global spread of bacterial resistance to drugs used in therapy requires new potent and safe antimicrobial agents. DNA gyrases represent important targets drug discovery. Schiff bases, thiazole, triazole derivatives are considered key scaffolds medicinal chemistry. Fifteen thiazolyl-triazole bases were evaluated for their antibacterial activity, measuring the growth inhibition zone diameter, minimum inhibitory concentration (MIC), bactericidal (MBC), against Gram-positive (Staphylococcus...
Background/Objectives: Angiogenesis plays a crucial role in tumor development and is driving force for the aggressiveness of several types cancer. Our team developed novel series thiosemicarbazone-containing quinazoline derivatives, TSC1-TSC10, as potential VEGFR2 inhibitors with proven anti-angiogenic antiproliferative potential. Methods: The TSC1-TSC10 was synthesized characterized by spectral data. Extensive methodology applied both vitro (Alamar Blue assay, Scratch CAM kinase assay)...
A series of 10 new N-phenyl-4-(4-(thiazol-2-yl)-phenyl)-thiazol-2-amine derivatives (3a–j) and 4 5-(2-(phenylamino)-thiazol-4-yl)-benzamide ethers (3′a–d) were synthesized from 4-(2-phenylamino)-thiazol-4-yl)-benzothioamide 2-hydroxy-5-(2-(phenylamino)-thiazol-4-yl)-benzamide with several α-halo-ketones, by the Hantzsch reaction. All compounds characterized elemental analysis spectral data (MS, FT-IR NMR). The final 14 substances screened for antimicrobial activity, against two...
New series of hydrazones 5–18 were synthesized, in good yields, by reacting 4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-carbohydrazide with differently substituted benzaldehyde. The resulting compounds characterized via elemental analysis, physico-chemical and spectral data. An antimicrobial screening was done, using Gram (+), (−) bacteria one fungal strain. Tested molecules displayed moderate-to-good growth inhibition activity. 2,2-Diphenyl-1-picrylhydrazide assay used to test the...
This study aims to evaluate the phenolic profile, and antioxidant antimicrobial activity of Achillea schurii Sch.-Bip., an endemic species from Romania that has not been investigated yet. The chromatographic profile components was obtained using HPLC-MS method, while total polyphenol, flavonoid, caffeic acid derivative contents were quantified spectrophotometric methods. evaluated different methods: DPPH radical scavenging, hemoglobin ascorbate peroxidase inhibition (HAPX), lipid...
In the context of there being a limited number clinically approved drugs for treatment Candida sp.-based infections, along with rapid development resistance to existing antifungals, two novel series 4-phenyl-1,3-thiazole and 2-hydrazinyl-4-phenyl-1,3-thiazole derivatives were synthesized tested in vitro their anti-Candida potential. Two compounds (7a 7e) showed promising inhibitory activity against pathogenic C. albicans strain, exhibiting substantially lower MIC values (7.81 μg/mL 3.9...
Schiff bases (SBs) are chemical compounds displaying a significant pharmacological potential. They able to modulate the activity of many enzymes involved in metabolism and found among antibacterial, antifungal, anti-inflammatory, antioxidant, antiproliferative drugs. A new thiazolyl-triazole SB was obtained characterized by elemental spectral analysis. The antibacterial antifungal ability evaluated against Gram-positive Gram-negative bacteria three Candida strains. showed good L....
In the context of dangerous phenomenon fungal resistance to available therapies, we present here chemical synthesis a new series thiazolyl-triazole Schiff bases B1–B15, which were in vitro assessed for their anti-Candida potential. Compound B10 was found be more potent against Candida spp. when compared with reference drugs Fluconazole and Ketoconazole. A docking study newly synthesized performed, results showed good binding affinity active site co-crystallized Itraconazole-lanosterol...
Twenty-three thiazolin-4-ones were synthesized starting from phenylthioamide or thiourea derivatives by condensation with α-monochloroacetic acid ethyl α-bromoacetate, followed substitution in position 5 various arylidene moieties. All the compounds physico-chemically characterized and IR (infrared spectra), 1H NMR (proton nuclear magnetic resonance), 13C (carbon resonance) MS (mass spectrometry) data consistent assigned structures. The thiazolin-4-one tested for antifungal properties...
This study aimed to investigate the polyphenolic composition and antioxidant antimicrobial potential of six Romanian Stachys species: S. officinalis, germanica, byzantina, sylvatica, palustris, recta. The LC-MS/MS method was used analyze profile, while phenolic contents were spectrophotometrically determined. activity evaluated using following methods: DPPH, FRAP, nitrite-induced autooxidation hemoglobin, inhibition cytochrome c-catalyzed lipid peroxidation, electron paramagnetic resonance...
Background and objectives: Cancer represents the miscommunication between within body cells. The mutations of oncogenes encoding MAPK pathways play an important role in development tumoral diseases. KRAS BRAF are involved colorectal cancer melanoma, while NRAS associated with melanoma. Thiazolidine-2,4-dione is a versatile scaffold medicinal chemistry useful tool new antitumoral compounds. aim our study was to predict pharmacokinetic/pharmacodynamic properties, drug-likeness lead-likeness...
Two series, “a” and “b”, each consisting of nine chemical compounds, with 2,3-disubstituted quinazolin-4(3H)-one scaffold, were synthesized evaluated for their anticonvulsant activity. They investigated as dual potential positive allosteric modulators the GABAA receptor at benzodiazepine binding site inhibitors carbonic anhydrase II. Quinazolin-4(3H)-one derivatives in vivo (D1–3 = 50, 100, 150 mg/kg, administered intraperitoneally) using pentylenetetrazole (PTZ)-induced seizure model mice,...
Lipophilicity, as one of the most important physicochemical parameters bioactive molecules, was investigated for twenty-two thiazolyl-carbonyl-thiosemicarbazides and thiazolyl-azoles. The determination carried out by reversed-phase thin-layer chromatography, using a binary isopropanol-water mobile phase. Chromatographically obtained lipophilicity were correlated with calculated log P D some biological parameters, determined in order to evaluate anti-inflammatory antioxidant potential...
A series of 12 new thiazolidine-2,4-dione derivatives were obtained by microwave-assisted synthesis. All compounds physicochemically characterized quantitative elemental C, H, N, S analysis and spectral data (mass spectrometry [MS], infrared [IR], nuclear magnetic resonance [NMR]), with the results being in agreement expected data. An vitro screening performed on Candida albicans ATCC 10231 showed their moderate antifungal activity, which was further investigated determining minimum...
Although Galanthus nivalis L. (snowdrop) is known for the galanthamine content, used in treatment of Alzheimer disease, polyphenolic compounds Amaryllidaceae species are less studied. Proper understanding polyphenolics these extracts and their antioxidant antimicrobial properties may allow a reconsideration medicinal uses.The content four selected harvested from Romania (Galanthus L., Narcissus pseudonarcissus N. poeticus Leucojum vernum L.) was determined by spectrophotometric methods;...
The rapid emergence of bacterial resistance to antibiotics currently available for treating infectious diseases requires effective antimicrobial agents with new structural profiles and mechanisms action. Twenty-three thiazolin-4-one derivatives were evaluated their antibacterial activity by determining the growth inhibition zone diameter, minimum inhibitory concentration (MIC), bactericidal (MBC), against gram-positive gram-negative bacteria. Compounds 3a–c, 3e–h, 6b–c 9a–c expressed better...
Abstract Balanites aegyptiaca is a tropical plant which widely used for medicinal purposes in several African countries, including Burkina Faso. Despite its widespread use, little known about phenolic content. This study sought to carry out screening of the polyphenols from leaves and galls B. aegyptiaca. A high-performance liquid chromatography–mass spectrometry method was investigate content parts studied here. The acid profile showed presence gentisic, p-coumaric, caffeic, ferulic sinapic...
A series of new 1,3,4‐oxadiazole/thiadiazole and 1,2,4‐triazole derivatives have been synthesized starting from 2‐aryl‐4‐methylthiazol‐5‐carbohydrazides isonicotinic acid hydrazide. All the newly compounds were characterized by IR, 1 H NMR, 13 C mass spectrometry. The screened for their antibacterial antifungal activity, assessed as growth inhibition diameter. Some them showed good activity against gram positive Staphylococcus aureus , while Listeria monocytogenes Escherichia coli Salmonella...