The aim of this study was rational design, synthesis and determination of physicochemical and pharmacological properties of series of new yhydroxybutyric acid (GHB) and y-butyrolactone (GBL) derivatives. The main part of the study was chemical synthesis of about hundred compounds utilizing different classical and modern methods, e.g. microwave-assisted organie synthesis (MAOS). For selected compounds various physicochemical descriptors were assigned with the use of computational and experimental methods as well. The pharmacological tests carried out as a part of the Anticonvulsant Screening Project (ASP, NIH, Rockville, USA) and in collaboration with Dept. of Pharmacodynamics of Jagiellonian University, revealed anticonvulsant and strong analgesic activity of some derivatives. Results of chemical and pharmacological investigations and SAR analysis led to select the most anticonvulsant and analgesic active compounds for further extending testing.
Jul 21, 2022
Nov 21, 2012
|ZB-109394||Jul 21, 2022|
Więckowski,Jarosław (red ). Strzyżewski,Krzysztof (red ).