443111-46-4Relevant academic research and scientific papers
Towards the rational design of novel drugs based on solubility, partitioning/distribution, biomimetic permeability and biological activity exemplified by 1,2,4-thiadiazole derivatives
Volkova,Terekhova,Silyukov,Proshin,Bauer-Brandl,Perlovich
, p. 162 - 175 (2017/02/05)
Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied.
5-Amino-3-(2-aminopropyl)-1,2,4-thiadiazoles as the basis of hybrid multifunctional compounds
Proshin,Serkov,Petrova,Bachurin
, p. 1148 - 1152 (2015/04/14)
An approach to the synthesis of hybrid multifunctional compounds starting from 1,2,4-thiadiazoles containing an amino group in the side chain was developed.
Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors: Approach to creation of bioavailable drugs
Perlovich, German L.,Proshin, Alexey N.,Volkova, Tatyana V.,Petrova, Ludmila N.,Bachurin, Sergey O.
experimental part, p. 2156 - 2167 (2012/10/08)
Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca uptake was measured. Permeation experiments on the phospholipid membranes were conducted, and the apparent
