A5045167164- Synthesis and biological activity
- Computational Drug Discovery Methods
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Circadian rhythm and melatonin
- Cholinesterase and Neurodegenerative Diseases
- Synthesis of Organic Compounds
- Tryptophan and brain disorders
- Tuberculosis Research and Epidemiology
- Alzheimer's disease research and treatments
- Chemical Reaction Mechanisms
- Multicomponent Synthesis of Heterocycles
- Neuroscience and Neuropharmacology Research
- Quinazolinone synthesis and applications
- Synthesis and Reactions of Organic Compounds
- Click Chemistry and Applications
- Cancer therapeutics and mechanisms
- Chemical Synthesis and Analysis
- Chemical synthesis and pharmacological studies
- Medicinal Plant Extracts Effects
- Stress Responses and Cortisol
- Mycobacterium research and diagnosis
- Synthesis and Characterization of Heterocyclic Compounds
- Bioactive Compounds and Antitumor Agents
- Phenothiazines and Benzothiazines Synthesis and Activities
Medical University of Sofia
2016-2025
Sofia University "St. Kliment Ohridski"
2015-2016
Bulgarian Academy of Sciences
2003-2004
A reduction in melatonin function contributes to the acceleration of Alzheimer's disease (AD), and understanding molecular processes melatonin-related signaling is critical for intervention AD progression. Recently, we synthesized a series analogues with donepezil fragments tested them silico vitro. In this study, one most potent compounds, 3c, was evaluated rat model pinealectomy (pin) followed by icvAβ1-42 infusion. Melatonin used as reference drug. Treatment 3c (10 mg/kg, i.p. 14 days)...
Alzheimer's disease (AD) is considered a complex neurodegenerative condition which warrants the development of multitargeted drugs to tackle key pathogenetic mechanisms disease. In this study, two novel series melatonin- and donepezil-based hybrid molecules with hydrazone (3a-r) or sulfonyl (5a-l) fragments were designed, synthesized, evaluated as multifunctional ligands against AD-related mechanisms. Two lead compounds (3c 3d) exhibited well-balanced profile, demonstrating intriguing...
Background/Objectives: New anti-tuberculosis compounds are needed to treat patients infected with multi- or extensively drug-resistant Mycobacterium tuberculosis strains. Studies based on spontaneous in vitro mutagenesis can provide insights into the possible modes of action and resistance mechanisms such new compounds. We evaluated primary response M. aroylhydrazones nitrofuroylamides. Methods: The reference strain H37Rv was cultured solid media at increased concentrations relative MIC....
Fifteen 4-methyl-1,2,3-thiadiazole-based hydrazone derivatives 3a–d and sulfonyl hydrazones 5a–k were synthesized. They characterized by 1H-NMR, 13C NMR, HRMS. Mycobacterium tuberculosis strain H37Rv was used to assess their antimycobacterial activity. All compounds demonstrated significant minimum inhibitory concentrations (MIC) from 0.07 0.32 µM, comparable those of isoniazid. The cytotoxicity evaluated using the standard MTT-dye reduction test against human embryonic kidney cells HEK-293T...
A reduction of melatonin function contributes to the acceleration Alzheimer's disease (AD), and understanding molecular processes melatonin-related signaling is critical for intervention AD progression. Recently, we synthesized tested a series derivates with donepezil fragments in silico vitro. In this study, one most potent compounds, 3c, was studied an vivo rat model pinealectomy (pin) subsequent icvAβ1-42 infusion. Melatonin used as referent drug. The treatment 3c (10 mg/kg, i.p....
Synthesized aminocoumarins are heterocyclic compounds possessing potential for the treatment of insulin-dependent diabetes mellitus with unexplored anti-glycative action. In this study 4-aminocoumarin derivatives (4-ACDs) were evaluated in vitro antiglycation (AG) activities by using human serum albumin (HSA)/glucose system, 8 weeks incubation. The glycation and conformational alteration HSA presence tested Congo red assay, fluorescence circular dichroism spectroscopy. antioxidant (AO)...
A plethora of pathophysiological events have been shown to play a synergistic role in neurodegeneration, revealing multiple potential targets for the pharmacological modulation Alzheimer's disease (AD). In continuation our previous work on new indole- and/or donepezil-based hybrids as neuroprotective agents, present study reports beneficial effects lead compounds series key pathognomonic features AD both cellular and vivo models. An enzyme-linked immunosorbent assay (ELISA) was used evaluate...
Breast cancer (BC) is the second leading cause of death in women, with more than 600,000 deaths annually. Despite progress that has been made early diagnosis and treatment this disease, there still a significant need for effective drugs fewer side effects. In present study, we derive QSAR models good predictive ability based on data from literature reveal relationships between chemical structures set arylsulfonylhydrazones their anticancer activity human ER+ breast adenocarcinoma...
Taking into consideration the arising resistance towards currently available antimycobacterial, there is still an unmet need for development of new chemotherapeutic agents to combat infectious agent. This study presents X-ray single-crystal analysis verify structure leading sulfonyl hydrazone 3b, which have proven their potent antimycobacterial activity against Mycobacterium tuberculosis H37Rv with MIC value 0.0716 μM, respectively, low cytotoxicity and very high selectivity indexes...
Based on the pharmacophore model of melatonin (MT1) receptor, we recently synthesized a series indole derivatives that showed anticonvulsant activity with low neurotoxicity and hepatotoxicity in rodents. In present study, three most potent C3-modified hydrazine structure 3c, 3e, 3f, 2-chlorophenyl, 2-furyl, 2-thienyl fragments, respectively, were selected, their neurobiological was explored mice. Experiment #1, dose-dependent anxiolytic effect single i.p. administration novel compounds at...
Reactions of 4-hydroxycoumarin (1a) and 4-chlorocoumarin-3-carbaldehyde (1b) with amino alcohols or alkylene diamines led to the formation corresponding N-substituted 4-aminocoumarins 3, 5 6. However, 4-hydroxycoumarin-3-carbaldehyde (8) reacted 2-aminoethanol ethylenediamine give 3-(aminomethylene)-chromane-2,4-diones 9a, b. The structure E-configuration compound 6 were proven by X-ray crystal analysis. Products b displayed signals both E- Z-isomers in their NMR spectra. All novel products...
A series of new thiazolidine-2,4-dione and hydantoin derivatives were synthesized by Knoevenagel condensation.. The compounds identified their melting points, 1H NMR, 13C HR-MS spectral data. in vitro antimycobacterial activity was evaluated against reference strain Mycobacterium tuberculosis H37Rv compared to that the first-line antituberculosis drugs isoniazid (INH) ethambutol (EMB). showed promising (MIC ranging from 0.75 1.54 µM) low cytotoxicity human embryonic kidney cell line HEK-293T...