[Synthesis and antibacterial activity of new polyfluoro-1,3,5-oxadiazines].

A number of polyfluro-3,6-dihydro-2H-1,3,5-oxadiazines and polyfluoro-4H-1,3,5-oxadiazines was designed. Relationship between their chemical structure and in vitro activity was investigated. The highest activity against grampositive microorganisms was shown by N1,N6-bis-[2,2,6,6-tetrakis(trifluoromethyl)-3,6-dihydro-2H-1,3,5-oxadiazine-4-yl]-1,6-hexane diamine.

[Synthesis of 1-hydroxyalkyl-3-substituted ureas and thioureas as a substrates for alcohol dehydrogenase]. / Sintez 1-gidroksialkil-3-zameshchennykh mochevin i tiomochevin kak substratov alkogol'degidrogenazy.

A series of 1-(2-hydroxyethyl)- and 1-(3-hydroxyethyl)-3-substituted ureas and thioureas were synthesized. 1-(3-Hydroxyethyl)-3-acylthioureas were shown to be specific substrates for alcohol dehydrogenase in vitro.

[Synthesis and antibacterial activity of the new 9-aminoacridine, 10,11-dihydro-5H-dibenzo[b,f]azepine, polyfluoro 5,6-dihydro-1,3,5-oxadiazine derivatives]. / Sintez i issledovanie antibacterial'noi aktivnosti novykh proizvodnykh 9-aminoakridina, 10,11-digidro-5H-dibenzo[b,f]azepina, poliftorirovannykh 5,6-digidro-1,3,5-oksadiazinov.

Screening among 9-aminoacridine, 10,11-dihydro-5H-dibenz[b, f]azepine and polyfluoro 5,6-dihydro-1,3,5-oxadiazine derivatives allowed to isolate compounds with potential antibacterial activity. Schemes of the active compounds synthesis are given. The most important is the estimation of the oxydiazines activity against gram-positive microorganisms including methicillin-resistant staphylococci. Special attention is paid to the activity of iminodibenzyl derivatives against multiresistant gram-negative microorganisms.

[Synthesis of uracil and theophylline derivatives and study of their effect on glucose transport in rat hepatic cells]. / Sintez proizvodnykh uratsila i teofillina i issledovanie ikh vliianiia na transport gliukozy v kletki pecheni krys.

A series of uracil and theophyllin derivatives were synthesized. 4-Amino-1,3-dimethyl-5-nonanoylaminouracil displayed the most pronounced effect of the in vitro stimulation of the 2-deoxyglucose transport into hepatic rat cells.

[Synthesis and antiproliferative activity of a novel N-acyl derivative of doxorubicin]. / Sintez i antiproliferativnaia aktivnost' novogo N-atsil'nogo proizvodnogo doksorubitsina.

Doxorubicin was acylated with estrone 3-hemisuccinate. The modified derivative exhibited high antiproliferative activity in vitro toward cell cultures of the MCF-7 human mammary adenocarcinoma and HepG2 human hepatoma.

[Effect of fluorine-containing ethers of permetrinic acid on inactivation kinetics of sodium influx into neuroblastoma cells (NEURO-2(alpha)]. / Vliianie ftorsoderzhashchikh éfirov permetrinovoi kisloty na kinetiku inaktivatsii natrievogo toka v kletkakh neiroblastomy (NEURO-2(alpha).

A synthesis of a number of esters of (+/-)-cis, trans-3-(2,2-dichlorovinyl) -2,2-dimethylcyclopropanecarboxylic acid with polyfluorinated alcohols was carried out. Their effect on kinetics of inactivation of sodium current in neuroblastoma (Neuro-2a) cells by the patch-clamp technique in the whole-cell configuration was investigated.

[The connection of the electronic structure and biological activity of various derivatives of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine]. / Sviaz' élektronnoi struktury i biologicheskoi aktivnosti nekotorykh proizvodnykh 1-metil-4-fenil-1,2,3,6-tetragidropiridina.

Electron structure of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and some of its analogs--the substrates of monoaminooxidase--substituted by phenyl cycles was studied by semiempiric quantum-chemical CNDOR, MINDOB methods. The relationship between the obtained electron and conformation parameters (orientation of the phenyl ring in particular) and biological activity of the compounds under consideration is discussed. A comparative analysis of the distribution pattern of the electron density for the MPTP molecule calculated by the above methods showed a good agreement between the results obtained.