A5044980627- Analytical Chemistry and Chromatography
- Phenothiazines and Benzothiazines Synthesis and Activities
- Pharmacogenetics and Drug Metabolism
- Neuroscience and Neuropharmacology Research
- Neurotransmitter Receptor Influence on Behavior
- Crystallization and Solubility Studies
- Treatment of Major Depression
- Receptor Mechanisms and Signaling
- Synthesis and Biological Evaluation
- HIV/AIDS drug development and treatment
- Cancer therapeutics and mechanisms
- Innovative Microfluidic and Catalytic Techniques Innovation
- Chemical Reaction Mechanisms
- Phosphodiesterase function and regulation
- Synthesis and pharmacology of benzodiazepine derivatives
- Synthesis and Reactivity of Heterocycles
- Microfluidic and Capillary Electrophoresis Applications
- Pharmacological Receptor Mechanisms and Effects
- Asymmetric Synthesis and Catalysis
- Computational Drug Discovery Methods
- Protein purification and stability
- X-ray Diffraction in Crystallography
- Chemical synthesis and alkaloids
Medical University of Warsaw
2015-2023
Instytut Farmaceutyczny
2015
Two series of novel 4-aryl-2H-pyrido[1,2-c]pyrimidine (6a–i) and 4-aryl-5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine (7a–i) derivatives were synthesized. The chemical structures the new compounds confirmed by 1H 13C NMR spectroscopy ESI-HRMS spectrometry. affinities all for 5-HT1A receptor serotonin transporter protein (SERT) determined in vitro radioligand binding assays. test demonstrated very high (6a–i 7a–i) generally low SERT protein, with exception 6a 7g. Extended affinity tests receptors...
Abstract A novel capillary electrophoresis method was developed for the determination of new 4-aryl-pyrido[1,2-c]pyrimidine derivatives, potential antidepressant agents, in serum. The derivatives have conformationally restricted tryptamine moiety pharmacophore portion and exhibit high affinity to molecular targets: 5-HT 1A receptor serotonin transporter protein. separation process conducted using an eCAP fused-silica capillary, detection wavelength 214 nm, 200 mM phosphate buffer adjusted pH...
This work is a continuation of our previous research, concentrating this time on lead structure modification to increase the 5-HT1A receptor affinity and water solubility designed compounds. Therefore, compounds synthesised within present project included structural analogues 3β-acylamine derivatives tropane with introduction methyl substituent in benzyl ring 2-quinoline, 3-quinoline, or 6-quinoline moiety. A series novel 3β-aminotropane was evaluated for their 5-HT1A, 5-HT2A, D2 receptors,...
Schizofrenia jest ciężką, przewlekłą chorobą psychiczną, dotykającą około 1% populacji. Staje się ona przyczyną skrócenia długości życia oraz wycofania z rodzinnego, społecznego i zawodowego. Różnorodność domen symptomatycznych, takich jak objawy pozytywne, negatywne kognitywne, wymaga kompleksowego podejścia do leczenia. Wyniki ostatnich badań na dużą skalę, porównujących leki pierwszej drugiej generacji, pokazały, że te drugie ani nie są skuteczniejsze, wiążą ze znaczącą poprawą funkcji...
This article describes the synthesis of new chiral 3-(piperidin-3-yl)-1H-indole derivatives (R)-10a-c and (S)-11a-c from corresponding diastereomers: (3R, 2R) (3S, 2R)-2-[3-(1H-indol-3-yl)-1-piperidyl]-2-phenyl-acetamides 2R)-4a, 2R)-6b, 2R)-8c 2R)-5a, 2R)-7b, 2R)-9c. Diastereomers were obtained by N-alkylation racemic 3-(piperidin-3-yl)-1H-indoles 1a-c using (S)-2-(4-toluenesulfonyloxy)-phenylacetic amide (S)–II. The same method was applied to obtain...