Perlovich German L, Proshin Alexey N, Volkova Tatyana V, Petrova Ludmila N, Bachurin Sergey O
Institute of Solution Chemistry, Russian Academy of Sciences , 153045 Ivanovo, Russia.
Mol Pharm. 2012 Aug 6;9(8):2156-67. doi: 10.1021/mp300011r. Epub 2012 Mar 6.
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.
合成并鉴定了新型1,2,4-噻二唑衍生物作为有效的神经保护剂。测定了它们抑制谷氨酸刺激的钙摄取的能力。进行了磷脂膜的渗透实验，并获得了表观渗透系数。测定了在正辛醇/缓冲液（pH 7.4）和正己烷/缓冲液（pH 7.4）不混溶相（作为表征胃肠道膜和血脑屏障的模型系统）中的分配系数。从“渗透-活性”性质的角度对所研究的化合物进行了分类。
