[Quantitative dependence of structure-antiseizure activity in a series of macrocyclic compounds]. / Kolichestvennaia zavisimost' struktura-protivosudorozhnaia aktivnost' v riadu makrotsiklicheskikh soedinenii.

In the present study we have further examined the influence of some structure parameters of macrocyclic polyethers upon their anticonvulsant activity in order to determine basic pharmacophore fragments. The anticonvulsant activity was studied experimentally for 25 new macrocyclic compounds, and their structure, physico-chemical properties, electron donor factors and atom charges were calculated using programs HyperChem-ChemPlus and HYBOT. The data about atomic properties were presented as a set functions of inter-atomic distances (Program MOLTRA). The cluster analysis revealed that studied compounds represent two independent groups which differ from chemical and pharmacological viewpoints. For first group, we have found that anticonvulsant activity of macrocycles is determined by their polarizability and spatial orientation of electron donor atoms. For another cluster the correlation was found between activity and spatial orientation of two hydrophobic fragments and electron donor atoms as well.

[Synthetic Ca++-dependent proton carrier]. / Sinteticheskii Ca++-zavisimyi perenoschik protonov.

Influence of 1,5-(3,3'-dimethylphosphate)diphenoxy-3-oxapentane (DDOP) on conductivity (G) of bilayers of common fabbit brain lipids is studied. It has been found that DDOP increases the bilayer conductivity in the presence of Ca++ and Mg++ (G-maximum at pH = 7.0) they do not act in the presence of K+, Na+. pK'DDOP, pK"DDOP values are equal to 1.2, and 7.7 respectively as determined by titration. Formation of "pseudomacrocyclic" DDOP structure is suggested. The role of Ca++, Mg++ ions seems to consist in lipophilisation of ionized forms of DDOP.