New derivatives of isoquinolin-1-ones have been obtained. It is established that these substances have low toxicity and significantly influence motor and research activity of mice. One compound, 3,3-pentamethylene-3,4-dihydroisoquinoline-1-one, possesses central analgesic activity.

С целью изучения противомикробной активности синтезированы моно- и бикватернизованные производные на основе α-пиридина, 2,2'-пиридила. Исследована противомикробная активность (ПМА) полученных соединений в отношении штаммов грамотрицательной кишечной палочки и грамположительного золотистого стафилококка. Установлена зависимость проявляемой ПМА от природы радикала и наличия кислорода между пиридильными кольцами. Максимальную ПМА в отношении изученных штаммов проявляет дибромид-2,3-бис-(N-додецилпиридиний-2'-ил)хиноксалина.

3-Methoxy-11-methylthio-D11-12-aza-D-homonorketoequilenine has been synthesized and its neurotropic activity has been evaluated. The compound (50 mg/kg) stimulates motor and exploratory activity in the open field test, reduces the immobilization time in behavioural despair test, and has a positive effect on passive avoidance learning. The analgesic properties of this compound are of particular interest. The synthesized compound in a dose of 50 mg/kg demonstrated a reliable analgesic effect in hot plate, hot plate on inflamed paw, and acetic acid induced writhing tests, the effect being comparable with that of analgin.

A series of 3-spiro[adamantane-2,3’-isoquinolines] have been synthesized and their neurotropic activity and cytotoxicity were evaluated. Two compounds with anxiolytic activity were found, one of which also showed antitumor activity in vitro .

С целью изучения противомикробной активности синтезированы моно- и бикватернизованные производные дипиридилэтана (этиленов). Исследована противомикробная активность (ПМА) полученных соединений в отношении штаммов грамотрицательной кишечной палочки и грамположительного золотистого стафилококка. Установлена зависимость проявляемой ПМА от природы радикала при атоме азота, положения этано- и этеномостиков между циклами относительно ониевых атомов азота, наличия сопряженной системы между ними. Максимальную ПМА проявляет бромид 1-(N-додецилпиридиний-4-ил)-2-(4-пиридил)этилена в отношении изученных штаммов (3,9 и 2,0 мкг/мл соответственно).

New phenethylamide derivatives have been obtained. It is established that the synthesized compounds have low toxicity and exhibit no central analgesic activity; some of them suppress the motor and research activity in mice.

Three-component condensation of veratrole, isobutylene oxide, and aliphatic ω-chloronitriles via the Ritter reaction leads to 1-(ω-chloroalkyl)-6,7-dimethoxy-3,3-dimethyl-3,4-dihydroisoquinolines, the reduction of which with NaBH4 yields benzoannelated azabicyclo[m.n.0]alkanes. The synthesized compounds have been tested for the hypotensive and antiaggregant activity

Reduction of 1-aryl-6,7-dimethoxy-3,3-dimethyl-3,4-dihydroisoquinolines (obtained by the three-component condensation of veratrole, isobutylene oxide, and aromatic nitriles) leads to the corresponding 1,2,3,4-tetrahydroisoquinolines. Hydrochlorides of the synthesized compounds were tested for anticoagulant activity.

A series of mono- and biquaternized derivatives of dipyridylethanes and dipyridylethylenes have been synthesized and char actertized with respect to antimicrobial activity. The new compounds exhibit structure-derpendent antimicrobial action upon Gram-negative E. coli and Gram-positive St. aureus species. Monoquaternized dipyridylethane and dipyridylethylene derivatives show a higher antimicrobial activity than the compounds with two onium nitrogen atoms; the derivatives of dipyridylethane are less active than the analogous derivatives of dipyridylethylene. A high antimicrobiasl activity (MIC ~ 1 mg/ml) was observed for 1[N-cetyl-(4-pyridinium)]-2-(4-pyridyl)ethylene.

2-( p -Hydroxyphenyl)-cyclohexyl- w -chlorocarboxamides were synthesized using the Ritter reaction and were reduced by LiAlH 4 to substituted 2-( p -hydroxyphenyl)-cyclohexylamines. Acute toxicity, analgesic, and antidepressant activity of the synthesized compounds were studied and their action on locomotion and exploration in open-field test was evaluated.

By reductive cyclization of substituted ω-chloroamides by LiAlH 4 were obtained 1-[1-( p -hydroxybenzyl-cyclohexyl]-piperidine and another homologs of phencyclidine, which were tested for analgetic activity.

Реакции замещенных аренов с изомасляным альдегидом и метилтиоционатом, дающие 1-метилтио-3,4-дигидроизохинолины. Обработка AcOH/AcONa приводит к соответствующим 2H-3,3-диметил-3,4-дигидроизохинолин-1-онам, которые обладают значительной противовоспалительной и анальгетической активностью.

A series of substituted 1-arylamino-3,4-dihydroisoquinolines have been synthesized using reactions of 1-methylthio-3,3-dimethyl-3,4-dihydroisoquinolines with substituted anilines and 2-aminothiazoles. The products were tested for analgesic and antiinflammatory activity.