title: Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors: approach to creation of bioavailable drugs.
abstract: 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 permeability coefficients were obtained. The partition coefficients in n-octanol/buffer (pH 7.4) and n-hexane/buffer (pH 7.4) immiscible phases (as model systems for characterizing gastrointestinal tract membranes and BBB) were determined. A classification of the studied compounds from the standpoint of "permeability-activity" properties was proposed.
authors.affiliation: Institute of Solution Chemistry, Russian Academy of Sciences , 153045 Ivanovo, Russia.
authors.forename: German L
authors.initials: GL
authors.lastname: Perlovich
authors.forename: Alexey N
authors.initials: AN
authors.lastname: Proshin
authors.forename: Tatyana V
authors.initials: TV
authors.lastname: Volkova
authors.forename: Ludmila N
authors.initials: LN
authors.lastname: Petrova
authors.forename: Sergey O
authors.initials: SO
authors.lastname: Bachurin
mesh_terms: D000818:Animals; D001682:Biological Availability; D002118:Calcium / Q000378:metabolism; D018698:Glutamic Acid / Q000494:pharmacology; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D010743:Phospholipids; D051381:Rats; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism; D013830:Thiadiazoles / Q000494:pharmacology*
chemical_list: D010743:Phospholipids; D013830:Thiadiazoles; D018698:Glutamic Acid; D002118:Calcium