Pyridoindolový derivát stobadín, [(-)-cis-2,8-dimetyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3b]-indol]je perspektívne antiarytmikum, antihistaminikum, anestetikum, antiulcerózum so schopnosťou vychytávať voľné kyslíkové radikály. Boli pripravené prodrug formy – N(5) - acylsubstituovaný stobadín – aktívnej substancie – stobadínu – pričom sa predpokladá, že sa v organizme budúhydrolyzovať a aktívna látka sa bude uvoľňovať vo vyšších koncentráciách v rôznych biologických tkanivách. Predkladaná práca sa zaoberá sledovaním kinetiky hydrolýzy 13 acylderivátov stobadínuv prostredí tlmivého roztoku o pH 7 pri teplote 70 °C a 75 °C spektrofotometricky v UF oblastispektra. Stanovené rýchlostné konštanty sa korelovali s dĺžkou postranného acylového reťazcaa hodnotami pKa študovaných látok. Stanovil sa profil log k – pH látok.

The pyridoindole derivative stobadin, [(-)-cis-2,8-dimetyl-2,3,4,4a,5,9b-hexahydro-lH-pyrido[4,3b]-indole] is a perspective antiarrhythmic, antihistamine, anaesthetic, antiulcerous drug capable of extinguishing free oxygen radical. Its prodrug forms - N(5)' acyl-substituted stobadine - of the active substance - stobadine - have been prepared and it is assumed that the will be hydrolyzed in the organism and the active substance will be released in higher concentrations in different biological tissues. The present paper is concerned with the investigation of the kinetics of the hydrolysis of 13 acyl derivatives of stobadine in the medium of a buffer solution of pH 7 at temperatures of 70 °C and 75 °C spectrophotometrically in the UV regioi ion of the spectrum. The determined rate constants were correlated with the length of the side acyl chain and the pKa values of the drugs under study. The profile of log k - pH of substances was determined.

Katedra farmaceutickej chémie Farmaceutickej fakulty Univ Kom Bratislava

Study of the kinetics of hydrolysis of stobadine acyl derivatives, the prodrug forms of extinguishers of free oxygen radicals. Part 3: hydrolysis in neutral medium

Štúdium kinetiky hydrolýzy acylderivátov stobadínu, prodrug foriem zhášačov voľných kyslíkových radikálov. 3. časť: hydrolýza v neutrálnom prostredí = Study of the kinetics of hydrolysis of stobadine acyl derivatives, the prodrug forms of extinguishers of free oxygen radicals. Part 3: hydrolysis in neutral medium /

Study of the kinetics of hydrolysis of stobadine acyl derivatives, the prodrug forms of extinguishers of free oxygen radicals. Part 3: hydrolysis in neutral medium /

Lit: 16

Souhrn: eng