Heteroarylaminoethanol derivates are drugs which affect sympathetic nervous system and are used for medications of hypertension. In solutions they behave like weak bases and their pK(a) values represent important information on their potential biological uptake, pharmacological activity and in vivo biodisponsibility. This article brings the measurement of pK(a) values of the series of seven new important heteroarylaminoethanols, compounds with potential vasodilating, beta-adrenolytic and antioxidant activity, by capillary zone electrophoresis (CZE) with diode-array detection. It has been shown that capillary zone electrophoresis measurements of pK(a) can be easily performed with very small quantities of studied substances, and, due to CZE separation power, the purity of samples is not of key importance. Moreover, the CZE method is fast and reliable, providing that suitable operational conditions are selected. The method is based on the measurement of the effective mobility curves within a suitable pH range and related regression analysis where pK(BH)(+) and electrophoretic mobility of BH(+) are explicitly involved. The selection of sufficient operational buffers is of key importance for accurate and reproducible results, and, this article brings step by step the consideration procedure involved in this process. Further, this paper brings principles of least square regression analysis of non-linear function corresponding to exact explicit formula for mobility curve of monovalent weak base.
- MeSH
- antihypertenziva chemická syntéza chemie MeSH
- chemické modely MeSH
- elektroforéza kapilární MeSH
- ethanolaminy chemická syntéza chemie MeSH
- farmaceutická technologie metody MeSH
- financování organizované MeSH
- koncentrace vodíkových iontů MeSH
- metoda nejmenších čtverců MeSH
- nelineární dynamika MeSH
- osmolární koncentrace MeSH
- pufry MeSH
- reprodukovatelnost výsledků MeSH
Pelvic inflammatory disease je celosvetovo významnou príčinou morbidity s potenciálnymi vážnymi komplikáciami. Infekcia má polymikrobiálnu etiológiu. Etiologicky sa na zápale podieľa hlavne Chlamydia trachomatis, Neisseria gonorrhoeae, anaeróbne gramnegatívne baktérie, zriedkavejšie mykoplazmy a ureaplazmy. Rutinný skríning asymptomatických chlamýdiových infekcií môže pomôcť v prevencii ochorenia.
Pelvic inflammatory disease (PID) remains a significant cause of morbidity worldwide, with the potential to result in serious complications. Infection has polymicrobial aetiology. Aetiologically, the main pathogens are Chlamydia trachomatis, Neisseria gonorrhoeae, anaerobic gram-negative rods less frequently Mycoplasma and Ureaplasma. Routine screening for asymptomatic chlamydial infection can help prevent disease.
Potenciometrická titrácia v zmesiach voda – metanol bola použitá na stanovenie zdanlivých ionizačných konštánt (w spKa) potenciálnych liečiv, 12 protonizovaných báz, alkylesterov kyseliny 2-, 3-, 4-{3-(4-difenylmetyl- -piperazin-1-yl)-2-hydroxy-propoxy}fenylkarbámovej vo forme dihydrochloridov. Hodnoty pKa pre vodné prostredie boli získané extrapoláciou závislosti Yasuda–Shedlovsky; zvolený postup bol overený použitím modelovej zlúčeniny trimekaín–hydrochloridu. Prvá ionizačná konštanta študovaných látok sa pohybovala v rozmedzí od 2,7 do 3,2, druhá od 6,5 do 7,2. V homologických radách bol pozorovaný len mierny pokles ionizačných konštánt s rastúcim počtom uhlíkov. Experimentálne získané pKa boli porovnané s disociačnými konštantami získanými výpočtovým programom SPARC.
Apparent ionization constants (w spKa) of potential drugs, a series of twelve protonated bases, 2-,3-,4-{3-(4- -benzhydryl-piperazine-1-yl)-2-hydroxy-propoxy}-phenylcarbamic acid alkylesters dihydrochlorides, were determined by automated potentiometric titrations in mixtures water – methanol. Aqueous pKa were assessed by means of Yasuda-Shedlovsky equation. Approach for pKa determination was evaluated using trimecaine hydrochloride as the model compound. The first values of ionization constants ranged approximately from 2.7 to 3.2, the second ones from 6.5 to 7.2. Only a slight decrease in ionization constants with the number of carbon atoms was observed in homological series. Experimentally determined dissociation constants were compared with the values predicted by the computer program SPARC.
- MeSH
- Basidiomycota imunologie MeSH
- dieta MeSH
- imunitní systém účinky léků MeSH
- karcinogeny imunologie MeSH
- krysa rodu rattus MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- zvířata MeSH
- Publikační typ
- srovnávací studie MeSH
- MeSH
- atrazin toxicita MeSH
- imunitní systém účinky léků MeSH
- imunotoxiny MeSH
- myši inbrední A MeSH
- myši MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- MeSH
- fenoxyacetáty imunologie toxicita MeSH
- herbicidy MeSH
- imunitní systém účinky léků MeSH
- imunosupresivní léčba MeSH
- myši MeSH
- testy toxicity metody MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- srovnávací studie MeSH
