piperidine OR C032727
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V práci prezentujeme výsledky analytického hodnotenia a štúdia niektorých fyzikálno-chemickýchvlastností potenciálneho liečiva CK-3635 s výrazným lokálne anestetickým účinkom. Štruktúralátky bola potvrdená IČ aUVspektroskopiou, stanovili sme teplotu topenia, rozpustnosť, rozdeľovacíkoeficient, kapacitný faktor, povrchovú aktivitu, disociačnú konštantu, študovali sme chromatografickésprávanie sa látky na Silufole®. Pre stanovenie obsahu látky v čistej substancii sme použilispektrofotometriu v ultrafialovej oblasti pri vlnovej dĺžke 234 nm, extrakčnú titráciu aniónaktívnymitenzidmi v dvojfázovom prostredí a vysokoúčinnú kvapalinovú chromatografiu.
The paper presents the results of analytical and pharmacological evaluation and study of somephysicochemical properties of a potential drug marked as CK-3635 with high local anaestheticactivity. The structure of the substance has been confirmed by IR and UV spectroscopy. The meltingpoint, solubility, partition coefficient, capacity factor, surface activity, and dissociation constant weredetermined. The chromatographic behaviour of the drug on a thin layer was also investigated. Forthe content determination, spectrophotometry in the ultraviolet region of the spectrum at thewavelenght of the second absorption maximum of the substance, the titration in the two-phasesambient, and high-performance liquid chromatography were used.
- MeSH
- anestetika lokální analýza chemie MeSH
- chemické techniky analytické metody MeSH
- chromatografie na tenké vrstvě metody MeSH
- farmaceutická chemie metody MeSH
- fyzikální chemie metody MeSH
- karbamáty analogy a deriváty analýza chemie MeSH
- spektrofotometrie ultrafialová metody MeSH
- techniky in vitro MeSH
A novel series of racemic piperidin-3-yl and piperidin-4-yl derivatives of nucleobases and their phosphonate derivatives were prepared.
- MeSH
- cisplatina analogy a deriváty farmakologie metabolismus MeSH
- DNA účinky léků MeSH
- finanční podpora výzkumu jako téma MeSH
- lidé MeSH
- ligandy MeSH
- piperidiny farmakologie chemie MeSH
- protinádorové látky farmakologie metabolismus MeSH
- vazebná místa MeSH
- Check Tag
- lidé MeSH
- ženské pohlaví MeSH
- Geografické názvy
- Španělsko MeSH
The development of biologically active molecules based on molecular recognition is an attractive and challenging task in medicinal chemistry and the molecules that can activate/deactivate certain receptors are of great medical interest. In this contribution, selected pyrimidine/piperidine derivatives were synthesized and tested for the ability to activate/deactivate Aryl hydrocarbon receptor (AhR) and Glucocorticoid receptor (GR). Tested compounds are shown to activate the receptors but to much lesser extent than positive controls, dioxin and dexamethasone for Ahr and GR, respectively. However, some of them antagonized the positive controls action. Although further in vivo studies are needed to fully characterize the bioactivities of these compounds, the reported in vitro evidences demonstrate that they might be used as the modulators of AhR and GR activities.
- MeSH
- buňky Hep G2 MeSH
- HeLa buňky MeSH
- lidé MeSH
- molekulární modely MeSH
- objevování léků MeSH
- piperidiny chemie farmakologie MeSH
- pyrimidiny chemie farmakologie MeSH
- receptory aromatických uhlovodíků agonisté antagonisté a inhibitory metabolismus MeSH
- receptory glukokortikoidů agonisté antagonisté a inhibitory metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Addition of lithiated methoxyallene to aziridine derivatives provided the expected primary addition products. The less substituted carbon of the aziridine ring was attacked selectively. The primary adducts could be converted to enantiopure piperidine derivatives or ß-amino acid derivatives. The unexpected reactions lead to a tricyclic sulfonamide and to alkynyl-substituted aminoethers. The efficient two-step conversion of a piperidone derivative to a benzomorphan demonstrates the potential of this approach to biologically active compounds.
