The reaction of substituted 1-aminoalkyl-3-hydroxy-3-pyrrolin-2-ones with hydrazine hydrate in boiling glacial acetic acid leads to the formation of 1-aminoalkyl-5,6-diaryl-2-oxopyrrolo[3,4-c]pyrazoles. The structure of the obtained compounds was confirmed by IR, 13C NMR and 1H NMR spectroscopy methods.

Short heating of a mixture of tryptamine, aromatic aldehyde and 4-methylbenzoylpyruvic acid methyl ester followed by keeping for 24 h at room temperature leads to the formation of 5-aryl-1-[2-(1H-indol-3-yl)ethyl]-4-(hydroxy-p-tolylmethylene)pyrrolidine-2,3-diones. Structure of the obtained compounds was confirmed by IR and 1H NMR spectroscopy methods. Antimicrobial activity of the obtained compounds was investigated.

Тропилированием иминов получены: N-бензилиден-4-(1-циклогепта-2,4,6-триенил)анилин (IIIa), N-(4-бромфенилметилен)-4 1 -(1-циклогепта-2,4,6-триенил)анилин (IIIb), N-(4-метоксифенилметилен)-4 1 -(1-циклогепта-2,4,6-триенил)анилин (IIIc). 4-(5-Дибензо[ a , d ]циклогептен-5-ил)анилин (V) получен реакцией анилина с дибензосуберенолом (VI), а N-бензилиден-4-(5-дибензо[ a , d ]циклогептен-5-ил)анилин (IV) из бензальанилина и соединения (V). Изучение их антимикобактериальной активности показало, что соединения IIIa, IIIc и IV обладают ингибирующим действием в отношении бактерий Staphylococcus aureus в концентрации > 1000 мкг/мл, соединения IIIa и V соответственно ингибируют рост бактерий Escherchia сoli или грибков Candida albicans в концентрации 1000 мгк/мл.

5-Aryl-4-acyl-3-hydroxy-1-[2-(imidazolyl-3-yl)ethyl]-3-pyrroline-2-ones were synthesized by three-component reaction of methyl dioxobutanoates with aromatic aldehydes and histamine dihydrochloride. Analgesic activity and hemostatic action of some compounds obtained was investigated.

A series of novel 5-(het)aryl-3-hydroxy-1-hydroxyethyl-4-(thienyl-2-carbonyl)-3-pyrrolin-2-ones was synthesized by reacting methyl thienyl-2-carbonylpyruvate with a mixture of aromatic or heterocyclic aldehyde and ethanolamine in dioxane. Antibacterial and antifungal activity of the synthesized compounds was studied.

A series of 1-(2-aminopropyl)-5-aryl-4-acyl-3-hydroxy-3-pyrrolin-2-ones were synthesized by three-component reactions of 4-substituted 2,4-dioxobutanoic acid methyl esters with mixtures of an aromatic aldehyde and 1,2-diaminopropane. Products of their reactions with hydrazine, p-phenetidine, and acetic anhydride were obtained. The analgesic, anti-inflammatory, and antimicrobial activities and hemostatic effect of several compounds were studied.

The article presents the review of initial stage of carried out studies of an analgetic activity of substituted 1-(2-imidazolethyl)-3-pyrroline-2-ons. We have established that compound marked with laboratory cipher as GKN-1165 at a dose of 50 mg/kg has analgetic activity close to the activity of ethanol of nimesulid comparison taken at the same dose.

5-Aryl-4-acyl-3-hydroxy-1-(2-piperazin-1-ylethyl)-2,5-dihydropyrrol-2-ones (I) were synthesized by reactions of methyl esters of acylpyruvic acids with a mixture of aromatic aldehyde and 2-(1-pyperazino)-1-ethylamine. Then, the corresponding hydrochlorides (II) were obtained. Compounds I were transformed to 3,4-diaryl-4,6-dihydro-6-oxo-5-(2-piperazin-1-ylethyl)pyrrolo[3,4- c ]pyrazol-6-ones (III) by reaction with hydrazine hydrate. The antibacterial activity of compounds I and the influence of compounds II and III on blood coagulation were studied and the acute toxicity of two compounds was evaluated.

5-Aryl-4-acyl-3-hydroxy-1-(2-piperazin-1-ylethyl)-2,5-dihydropyrrol-2-ones (I) were synthesized by reactions of acylpyruvate methyl esters with a mixture of aromatic aldehyde and 2-(1-piperazino)-1-ethylamine. Then, the corresponding hydrochlorides (II) were obtained. Compounds I were transformed into 3,4-diaryl-4,6-dihydro-5-(2-piperazin-1-ylethyl)pyrrolo[3,4-c]pyrazol-6-ones (III) by reaction with hydrazine hydrate. The antimicrobial activity of compounds I and the influence of compounds II and III on blood coagulation were studied. The acute toxicity of two compounds was evaluated.

The reactions of methyl 2,4-dioxo-4-phenylbutanoate and methyl 2,4-dioxopentanoate with a mixture of an aromatic aldehyde and propane-1,2-diamine, depending on the initial reactant ratio, gave 4-acyl-1-(2-aminopropyl)-5-aryl-3-hydroxy-2,5-dihydro-1H-pyrrol-2-ones and 1,1′-(propane-1,2-diyl)bis(4-acetyl-3-hydroxy-5-phenyl-2,5-dihydro-1H-pyrrol-2-one). Reactions of substituted 1-(2-aminopropyl)-2,5-dihydro-1H-pyrrol-2-ones with aromatic amines and hydrazines were studied, and the structure of one of the products, 5-(2-aminopropyl)-3,4-diphenylpyrrolo[3,4-c]pyrazol-6-one, was proved by X-ray analysis.

Interaction of methyl esters of acylpyruvic acides with mixture of aromatic aldehyde and tryptamine or 5-methoxytryptamine leads to 5-aryl-4-acyl-3-hydroxy-1-[2-(3-indolil)-ethyl)-2,5-dihydropyrrol-2-ones (I). The compounds (I) were transformed to 3,4-diaryl-1,4,5,6-tetrahydro-6-oxo-5-(2-(3-indolil)-ethyl)pyrrolo[3,4-c]pyrazoles (II) by reaction with hydrazine-hydrate. The structure of received compounds is established. The analgetical activity of compounds (I б-е) and (II) is investigated.

A series of 5-aryl-4-acyl-3-hydroxy-1-morpholinoalkyl-3-pyrroline-2-ones was synthesized via the reactions of methyl esters of acylpyruvic acids with a mixture of aromatic aldehyde and 2-(4-morpholino)-1-ethylamine or 3-(4-morpholino)-1-propylamine. All compounds possess weak antibacterial properties. The antiamnesic, analgesic, and antiphlogistic activity and acute toxicity of several compounds were studied. It was established that one compound produced a significant antiamnesic effect and two compounds exhibited pronounced analgesic activity.

1-(3-Aminopropyl)-5-aryl-4-acyl-3-hydroxy-3-pyrrolin-2-ones (I–X) were prepared via reaction of methyl acylpyruvates and a mixture of aromatic aldehyde and 1,3-diaminopropane in a 1:1:1 molar ratio. The products were converted to hydrochlorides XI–XV in 48–90% yields. 1,3-Di(4-acetyl-3-hydroxy-2-oxo-5-phenyl-3-pyrrolin-1-yl)propane (XVI) was produced in 16% yield via reaction of methyl acetylpyruvate with a mixture of benzaldehyde and 1,3-diaminopropane in a 2:2:1 molar ratio. The biological activity of the 12 products was studied.

The interaction of methyl esters of acylpyruvic acids with a mixture aromatic aldehyde and 1,3-diaminopropane in a molar ratio 1:1:1 leads to 1-(3-aminopropil)-5-aryl-4-acyl-3-hydroxy-3-pyrroline-2-ones (I - X), which can be subsequently transformed into hydrochlorides (XI - XV) with yields within 48 - 90 %. The interaction of methyl ether of acylpyruvic acid with a mixture benzaldehyde and 1,3-diaminopropane in a molar ratio 2:2:1 lead to 1,3-di(4-acetyl-3-hydroxy-2-okso-5-phenyl-3-pyrrolin-1-yl)propane (XVI) with a yield of 16 %. The biological activity of the synthesized compounds has been studied,

Reactions of methyl ethers of acylpyruvic acids with a mixture of aromatic aldehyde and 2-methoxyethylamine or 3-isopropoxypropylamine were used to synthesize a series of 1-alcoxyalkyl-5-aryl-4-acyl-3-hydroxy-3-pyrrolin-2-ones possessing antibacterial activity.

Reactions of methyl ethers of acylpyruvic acids with a mixture of aromatic aldehyde and 2-methoxyethylamine or 3-isopropoxypropilamine were used to synthesize a series of 1-alcoxyalkil-5-aryl-4-acyl-3-hydroxy-3-pyrrolin-2-ones possessing antibacterial activity.

Реакцией метиловых эфиров ацилпировиноградных кислот со смесью ароматического альдегида и 2-(4-морфолино)-1-этиламина или 3-(4-морфолино)-1-пропиламина синтезированы 5-арил-4-ацил-3-гидрокси-1-морфолиноалкил-3-пирролин-2-оны (I - XXXVI), проявляющие слабую антимикробную активность. У нескольких соединений исследованы антиамнестическое, анальгетическое, противовоспалительное действие и острая токсичность. Выявлено одно соединение с выраженной ноотропной и два - с анальгетической активностью.