R. V. Paronikyan

Synthesis and Antibacterial Activity of Oxalates and Acetamides of {2-[2-Sopropyltetrahydropyran-4-yl-4-(4-Fluorophenyl)]Ethyl}Arylamines

The reaction of cyano(2-isopropyltetrahydropyran-4-ylidene)acetic acid ethyl ester and 4-fluorophenylmagnesium bromide produced the cyanoester that was decarboxylated to the corresponding nitrile. Reduction of the latter by LiAlH4 formed 2-[4-(4-fluorophenyl)-2-isopropyltetrahydropyran-4-yl]ethylamine, reaction of which with aromatic aldehydes synthesized azomethines that were then reduced by NaBH4 to secondary amines. The last were transformed to oxalates and acetamides. It was shown that the secondary amine oxalates possessed high antibacterial activity.

Synthesis and Antitumor and Antibacterial Properties of New N-Alkylated Pyrimidines

Uracil and 5-fluoro-, -bromo-, and -iodouracils were alkylated by substituted benzylchlorides to obtain N1-mono- and N1,N3-bis-substituted derivatives. The toxicity, antitumor, and antibacterial properties of the synthesized compounds were investigated. It was established that 5-fluoro- and 5-iodouracils exhibited more pronounced antitumor properties than 5-bromouracil derivatives.

Synthesis and antibacterial properties of hydrazonothiazolyl derivatives of saturated 2,4,4-substituted butanolides

A method has been developed for the synthesis of new heterocyclic compounds containing γ-butanolide fragments. The antibacterial properties of the obtained compounds have been investigated. The tested compounds exhibit moderate antibacterial activity.

Synthesis, Transformations, and Study of Some Biological Properties of New 3,4,5-Substituted 1,2,4-Triazoles

A series of new 3,4,5-substituted 1,2,4-triazoles were synthesized. Their SH-alkylation by various alkylating compounds and aminomethylation leading to the formation of Mannich bases were studied. The influence of the synthesized compounds on the level of DNA methylation and their antitumor and antibacterial properties were investigated. Several compounds with pronounced demethylation and weak antitumor and antibacterial activities were identified. Correlations among the investigated biological properties were not found.

Synthesis and biological properties of new derivatives of 2-arylpyrrolidinecarbonitriles and pyrrolidinecarboxamides

A series of new analogs of 2-arylpyrrolidinecarbonitriles were synthesized under phase-transfer catalysis conditions. New analogs of pyrrolidinecarboxamides were synthesized based on these carbonitriles. Biological evaluation showed that the synthesized derivatives of pyrrolidinecarbonitriles and pyrrolidinecarboxamides possessed moderate anticancer activity.

Synthesis and biological activity of substituted 6-alkyl(6H)-3-phenyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines

A series of substituted 6-alkyl(6H)-3-phenyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines have been synthesized by reaction of 3-alkyl-4-amino-5-thio-1,2,4-triazoles with substituted phenacylbromides in the presence of an equimolar amount of KOH. Mass spectra for the dissociative ionization by electron impact, antibacterial activity, and antitumor properties of the synthesized compounds have been studied. It was established that some compounds at doses of 50 – 100 mg/kg decrease the growth of sarcomas 45 and 37 by 35 – 47%.

Synthesis and Antibacterial Properties of Several Unsaturated Quaternary Ammonium Salts

A series of ammonium salts with various functional groups were synthesized by the reaction of the corresponding tertiary amines and alkyl halides. It was established that nine compounds (of ten synthesized) displayed bactericidal activity.

Synthesis and antibacterial activity of N-amino-derivatives of condensed pyridines

A method based on condensed 4-cyanopyridinethiones using O-tosylhydroxylamine as the aminating agent was developed for preparing tosylates of N-amino-derivatives of pyrano[3,4-c]pyridines; 5,6,7,8-tetrahydroisoquinolines; and cyclopenta[c]pyridines. The antibacterial activity of the synthesized compounds was assessed.

Synthesis and antibacterial activity of new 2.5-dihydrofuran derivatives

Aseries of new 2.5-dihydrofuran derivatives containing cyclohexyl rings have been synthesized. The antibacterial activity of these compounds has been investigated. The experimental results showed that some compounds exhibited moderate antibacterial activity with respect to both Gram-positive and Gram-negative bacterial species.

Synthesis and biological activity of pyrano[4,3-d]furo[2,3-b]pyridine derivatives

Furopyridines have a wide spectrum of biological activity [1 3] and some of them are used in medicine [4], thus stimulating a search for biologically active compounds among the derivatives of a new heterocyclic system, pyrano[4,3d]furo[2,3-b]pyridine. Synthesis was performed on the basis of 3-phenacyloxy-4-cyanopyrano[3,4-c]pyridines ( I a u) obtained earlier [5]. The presence of an active methylene group in these compounds makes it possible to carry out intramolecular cyclization in the presence of sodium ethylate, which yields 9-aminopyrano[4,3-d]furo[2,3-b]pyridines ( I I a u).