A5017003587- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Synthesis and biological activity
- Organophosphorus compounds synthesis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Biological Evaluation
- Nerve injury and regeneration
- Neurogenesis and neuroplasticity mechanisms
- HIV/AIDS drug development and treatment
- Parasites and Host Interactions
- Phosphorus compounds and reactions
- HIV Research and Treatment
- Click Chemistry and Applications
- Estrogen and related hormone effects
- Neuropeptides and Animal Physiology
- Receptor Mechanisms and Signaling
- Ion Transport and Channel Regulation
- Bioactive Compounds and Antitumor Agents
- Chemical Synthesis and Analysis
- Stress Responses and Cortisol
- Computational Drug Discovery Methods
- Pneumocystis jirovecii pneumonia detection and treatment
- Synthesis and Characterization of Heterocyclic Compounds
- ATP Synthase and ATPases Research
- Fluorine in Organic Chemistry
National Hellenic Research Foundation
2016-2025
Bridge University
2024
National Technical University of Athens
2014
National and Kapodistrian University of Athens
1996-2009
Hungarian Academy of Sciences
2005-2009
University of Szeged
2009
University of Crete
2003-2008
University College London
2006
Aristotle University of Thessaloniki
2001
Rega Institute for Medical Research
2001
The neurosteroid dehydroepiandrosterone (DHEA), produced by neurons and glia, affects multiple processes in the brain, including neuronal survival neurogenesis during development aging. We provide evidence that DHEA interacts with pro-survival TrkA pro-death p75NTR membrane receptors of neurotrophin nerve growth factor (NGF), acting as a neurotrophic factor: (1) anti-apoptotic effects were reversed siRNA against or specific inhibitor; (2) [3H]-DHEA binding assays showed it bound to membranes...
6H-Isoindolo[2,1-a]indoles (5, 7, 10, 13), 5,6-dihydroindolo[2, 1-a]isoquinolines (20, 21), and 6,7-dihydro-5H-benzo[c]azepino[2, 1-a]indoles (23, 25, 27, 30) have been prepared as melatonin analogues to investigate the nature of binding site receptor. The affinity was determined in a radioligand assay using cloned human mt(1) MT(2) receptor subtypes expressed NIH 3T3 cells. Agonist antagonist potency measured pigment aggregation response clonal line Xenopus laevis melanophores....
Sodium potassium pump (Na+/K+ ATPase) is a transmembrane protein complex found in all higher eukaryotes acting as key energy-consuming maintaining ionic and osmotic balance cells. Recently recognized an important transducer and/or integrator of various signals well protein-protein interaction scaffold forming receptor complexes with signaling properties, the most prominent pharmacological role Na+/K+ ATPase inhibitors increase myocardial contractility pathologic conditions such congestive...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of .beta.-keto phosphonates from vinyl phosphates via a 1,3-phosphorus migrationTheodora Calogeropoulou, Gerald B. Hammond, and David F. WiemerCite this: J. Org. Chem. 1987, 52, 19, 4185–4190Publication Date (Print):September 1, 1987Publication History Published online1 May 2002Published inissue 1 September 1987https://pubs.acs.org/doi/10.1021/jo00228a008https://doi.org/10.1021/jo00228a008research-articleACS PublicationsRequest reuse...
The aim of this study was to evaluate miltefosine and four synthetic compounds (TCAN26, TC19, TC106 TC117) for their in vitro inhibitory activity against Candida albicans planktonic biofilm cells investigate whether these are able inhibit the formation reduce viability mature C. cells. XTT reduction assay transmission scanning electron microscopy were employed determine effects test comparison with amphotericin B fluconazole both sessile biofilms. susceptible miltefosine, TCAN26 all...
Background The search for novel chemical entities targeting essential and parasite-specific pathways is considered a priority neglected diseases such as trypanosomiasis leishmaniasis. thiol-dependent redox metabolism of trypanosomatids relies on bis-glutathionylspermidine [trypanothione, T(SH)2], low molecular mass cosubstrate absent in the host. In pathogenic trypanosomatids, single enzyme, trypanothione synthetase (TryS), catalyzes biosynthesis, which indispensable parasite survival. Thus,...
The neurosteroid dehydroepiandrosterone (DHEA) at 1 nM protects NMDA-/GABAA-receptor negative neural crest-derived PC12 cells from apoptosis. We now report that membrane-impermeable DHEA-BSA conjugate replaces unconjugated DHEA in protecting serum-deprived apoptosis (IC50=1.5 nM). Protection involves phosphorylation of the prosurvival factor Src and induction anti-apoptotic protein Bcl-2 is sensitive to pertussis toxin. Binding assays [3H]DHEA on isolated cell membranes revealed saturation...
Abstract Self‐assembling chemotherapeutic agents are mixtures of relatively nontoxic precursors that can combine chemically under physiological conditions to form products with greater cytotoxic and/or antimicrobial activity than either the precursors. Combinations more rapidly in or near target (tumor, pathogen, virally infected cell) normal tissues will exhibit target‐selective synergism, thus exhibiting an antitarget selectivity is selectivities product (e.g., a hydrazone) and precursor...
6-Hydroxy-5,7,8-trimethyl-benzopyran derivatives and 5,7,8-trimethyl-1,4-benzoxazine analogues substituted by the lidocaine pharmacophore aminoamide functionality at C4 or N4, respectively, were synthesized evaluated against arrhythmias associated with ischemia−reperfusion injury. The antiarrhythmic effect of substitutents positions C2 C6 was examined. Six out 11 new derivatives, exhibited arrhythmia scores 1.0−1.3 versus control (4.5 ± 1.2), which also reflected to % premature beats...
DHEA analogues with modifications at positions C3 or C17 were synthesized and evaluated for neuroprotective activity against the neural-crest-derived PC12 cell model of serum deprivation-induced apoptosis. The most potent compounds spiro-epoxy derivatives 17β-spiro[5-androstene-17,2′-oxiran]-3β-ol (20), (20S)-3β,21-dihydroxy-17β,20-epoxy-5-pregnene (23), (20R)-3β,21-dihydroxy-17α,20-epoxy-5-pregnene (27) IC50 values 0.19 ± 0.01, 99.0 4.6, 6.4 0.3 nM, respectively. Analogues 20, 23, 27, up to...
Two series of novel ether phospholipids (EPs) have been synthesized. The first includes cyclodecylidene- or cyclopentadecylidene-substituted EPs carrying N,N,N-trimethylammonium N-methylpiperidino N-methylmorpholino head groups. second encompasses more rigid groups in combination with cycloalkylidene moieties the lipid portion. In addition, hydrogenated derivatives were obtained. All new analogues, except 33, 1.5- to 62-fold potent than miltefosine against intracellular L. infantum, and most...
Neurotrophin receptors mediate a plethora of signals affecting neuronal survival. The p75 pan-neurotrophin receptor controls cell fate after its selective activation by immature and mature isoforms all neurotrophins. It also exerts pleiotropic effects interacting with variety ligands in different or non-neuronal cells. In the present study, we explored biophysical functional interactions blood-brain-barrier (BBB) permeable, C17-spiroepoxy steroid derivative, BNN27, p75NTR receptor. BNN27 was...
Abstract Drug development is an arduous procedure, necessitating testing the interaction of a large number potential candidates with interacting (macro)molecules. Therefore, any method which could provide initial screening candidate drugs might be interest for acceleration by highlighting interesting compounds, prior to in vitro and vivo validation. In this line, we present may identify hits, agonistic and/or antagonistic properties on GPCR receptors, integrating knowledge signaling events...
Abstract Background Neural stem cell (NSC) proliferation and differentiation in the mammalian brain decreases to minimal levels postnatally. Nevertheless, neurogenic niches persist adult cortex hippocampus rodents, primates humans, with NSC sharing key regulatory mechanisms development. Adult neurogenesis impairments have been linked Alzheimer’s disease (AD) pathology. Addressing these by using neurotrophic factors is a promising new avenue for therapeutic intervention based on neurogenesis....
BACKGROUND Miltefosine (MIL) is the only oral drug approved for leishmaniasis treatment, but its use limited by gastrointestinal toxicity. Novel alkylphospholipid analogues may provide safer and more effective alternatives. OBJECTIVES This study aimed to assess antileishmanial activity, cytotoxicity, membrane interactions of three MIL TC387, TC388, TC437 against Leishmania amazonensis. METHODS Antileishmanial cytotoxic activities were evaluated in L. amazonensis, J774.A1 macrophages,...
A series of new compounds that contain lipoic acid and trolox connected through spacers were synthesized examined for their antioxidant activity protective effects against reperfusion arrhythmias in isolated heart preparations. All tested are strong inhibitors lipid peroxidation rat liver microsomal membranes induced by ferrous ions ascorbate. N-(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-carbonyl)-N'-(1,2-dithiolane-3-pentanoyl)-1,2-phenylenediamine (13) exhibits anti-lipid...
A series of well-defined poly[(ethylene oxide)-b-2-(dimethylamino)ethyl methacrylate] (PEO-b-PDMAEMA) diblock copolymers were synthesized by atom transfer radical polymerization (ATRP) techniques. Post-polymerization reactions performed to transform a portion the tertiary amine groups PDMAΕMA into phosphorozwitterions. The aggregation behavior prepared zwitterionic block was investigated static and dynamic light scattering techniques at 25 37 °C, in weakly basic acidic aqueous solutions....
Sodium potassium pump (Na(+)/K(+)ATPase) is a validated pharmacological target for the treatment of congestive heart failure. Recent data with inotropic drugs such as digoxin & digitoxin (digitalis) suggest potent anti-cancer action these and promote Na(+)/K(+)ATPase novel therapeutic in cancer. However, digitalis have narrow indices, are pro-arrhythmic considered non-developable by pharmaceutical industry. On contrary, series recently-developed steroidal inhibitors showed better properties...