The mechanisms of retention and separation of the enantiomers of chiral oxazolopyrroloquinolones on a stationary phase with graftеd macrocyclic antibiotic ristocetin A under conditions of high-performance liquid chromatography with aqueous methanol mobile phases have been studied. The retention factor was found to decrease monotonically when the CH 3 OH concentration in the mobile phase increased to 90 vol %; then it slightly increased as the composition of the mobile phase approached pure methanol. The thermodynamics of adsorption of oxazolopyrroloquinolones in different regions of this dependence was studied. A mathematical model has been proposed; it describes well the experimental data and allows for analyte solvation in the mobile phase and competitive adsorption (with mobile phase components) on a chiral selector. The results were compared with previously obtained data for water–acetonitrile mobile phases. The reasons for the observed differences were discussed.

Considering the side effects of existing drugs used for pain relief, the search for new analgesics with high efficacy and safety remains relevant. Aseries of imidazopyrrolo[3,4-b]quinoline-5,11-diones and pyrimidopyrrolo[3,4-b]quinoline-6,12-diones II were synthesized, whose analgesic activity at a dose of 0.05 mmol/kg was studied in the hotplate test in rats after i.p. administration. One compound was found with analgesic activity comparable to that of reference compound diclofenac sodium. Compounds II were less toxic than diclofenac sodium.

Учитывая побочные эффекты существующих лекарственных препаратов, назначающихся для избавления от боли, поиск новых анальгетиков, отличающихся высокой эффективностью и безопасностью, является актуальным. Синтезирован ряд имидазопирроло[3,4-b]хинолин-5,11-дионов и пиримидопирроло[3,4-b]хинолин-6,12-дионов II, анальгетическая активность которых в дозе 0,05 ммоль/кг изучалась в тесте «горячая пластинка» на крысах при внутрибрюшинном способе введения. Было выявлено одно соединение, анальгетическая активность которого сопоставима по эффекту с препаратом сравнения — диклофенаком натрия. Установлено, что соединения II менее токсичны, чем диклофенак натрия.

Thermal decarbonylation of methyl 1-aryl-3-(het)aroyl-4,5-dioxo-4,5-dihydro-1 H -pyrrole-2-carboxylates afforded 8-substituted methyl 3-(het)aroyl-4-oxo-1,4-dihydroquinoline-2-carboxylates. X-ray diffraction studies revealed no hydrogen bonds in the crystals of the compounds obtained. According to spectral data, hydrogen bonding is possible in concentrated solutions of 8-substituted methyl 4-oxo-1,4-dihydroquinoline-2-carboxylates.

Data on methods for the construction of the 4-quinolone skeleton and modification of the substituents around it are reviewed. The “structure–activity” relationships of 4-quinolones are examined with respect to antibacterial and antitumor activity.

Synthesis of a small library of compounds containing an aminovinylketone fragment is described. Results of studying their antibacterial activity against S. aureus ATCC 6538-P and E. coli ATCC 25922 are reported.

Synthesis of a small library of compounds containing aminovinylketone fragment is described and results of studying their antibacterial activity against St. aureus ATSS 6538-P and E. coli ATSS 25922 are presented.

Synthesis of small libraries of compounds containing 4-quinolone fragment and results of studying their antibacterial activity against S. aureus АТСС 6538-Р, E.coli АТСС 25922 are described.

Pharmacological activity of a series of new amino derivatives of dehydroabietic acid has been studied. 12-N,N-Diethylaminoacetyl-8,11,13-abietatrien-18-oate hydrochloride produces a calming effect, shows a pronounced anxiolytic activity, and exhibits antipyretic action comparable to that of the reference drug (analgin).

The biological activity of a series of new amino derivatives of dehydroabietic acid has been studied. 12-N,N-Diethylaminoacetyl-8,11,13-abietatrien-18-oate hydrochloride produces a calming effect, shows pronounced anxiolytic activity, and exhibits antipyretic action comparable with that of the reference drug (analgin).