Design and synthesis of substances regulating the activity of the cardiovascular system

Design and synthesis of compounds, regulating the activity of the cardiovascular system

Head of the Laboratory

Aghekyan Asya, Candidate of Chemical Sciences

ORСID: ID 0000-0001-6151-4951

Telephone: (+37410) 285–101

Research Directions

The laboratory focuses on the synthesis of novel compounds with antihypoxic, antiarrhithmic, antioxidant, antimonoaminoxidase, anticonvulsant and antimicrobial activity in the series of tetrahydroisoquinoline, 1,3-benzodioxole, 1,4-benzodioxane and five-membered heterocycles with two or three heteroatoms.

The main direction of the laboratory’s research is the synthesis of new oxygen- and nitrogen-containing heterocyclic compounds that regulate the activity of the cardiovascular and central nervous systems, as well as possessing antimicrobial, antihypoxic, antimonoaminoxidase, anticonvulsant and antioxidant activity, among 1,4-benzodioxane, 4-spiro-substituted tetrahydroisoquinoline and its non-cyclized analogues.

History of the Laboratory. Founded and headed by Varduhi Afrikyan, Candidate of Chemical Sciences, in 1955. The laboratory was engaged in the synthesis of new aromatic and heterocyclic amino ethers affecting the cardiovascular system and the study of their biological properties, with the aim of revealing the relationship between chemical structure and biological activity. As a result of biological research, a number of drugs were discovered: Fubromegan, Quateron and Gangleron, which have found wide application in medical practice.

In 1970, the laboratory was headed by Doctor of Chemical Sciences, Professor Eduard Margaryan, who, expanding the scope of the research, began work in the field of synthesis of diarylpropionic acids, arylalkylamines, condensed heterocyclic systems: indole, isoquinoline, benzazepine, benzodioxane, isochroman derivatives. As a result, a number of potential drugs were discovered: Fobufol, Difalkin, Emacor, Beditin, Mesedin.

Since 2011, the laboratory has been headed by Asya Aghekyan, Candidate of Chemical Sciences, who has continued the main direction of research – the targeted synthesis of biologically active compounds from nitrogen- and oxygen-containing heterocyclic annelated systems. The results of this work have been presented in numerous scientific publications.

Current activities

The laboratory employs 8 highly qualified specialists, including 4 PhD

Best Results

✔ Optimal conditions were developed for the synthesis of 4-spirocycloalkane-substituted tetrahydroisoquinoline derivatives containing at the second position amino- and sulfanylamide, alkanol and heterylalkyl pharmacophore fragments

Russ. J. Org. Chem., 2013, v. 49, No. 11, pp. 1632-1636. doi: 10.1134/S1070428013110122

Russ. J. Org. Chem., 2016, v. 52, No. 5, pp. 689-693. doi:10.1134/S1070428016050122

Russ. J. Org. Chem., 2022, v. 58, No. 11, pp. 1581-1588. doi:10.1134/S1070428022110045

Russ. J. Org. Chem., 2019, v. 55, No. 3, pp. 302-307. doi:10.1134/S1070428019030047

Russ. J. Org. Chem., 2015, v. 51, No. 2, pp. 221-225. doi:10.1134/S1070428015020153

✔ A new approach for the synthesis of tetrahydroisoquinoline derivatives containing two methyl groups at the fourth position based on substituted benzylamines has been proposed.

Russ. J. Org. Chem., 2017, v. 53, No. 3, pp. 362-365. doi:10.1134/S1070428017030083

Russ. J. Org. Chem., 2022, v. 58, No. 10, pp. 1409-1415. doi:10.1134/S1070428022100049

✔ Methods for the synthesis of various derivatives of 1,4-benzodioxane containing at the second position a substituted 1,2,4-triazole ring have been developed.

Russ. J. Org. Chem., 2017, v. 53, No. 3, pp. 428-432. doi:10.1134/S1070428017030198

Russ. J. Gen. Chem., 2018, v. 88, No. 4, pp. 839-842. doi:10.1134/S1070363218040345

Russ. J. Org. Chem., 2020, v. 56, No. 3, pp. 436-439. doi:10.1134/S1070428020030112

Chem. J. Armenia, 2023, v. 76 № 1-2, pp. 104-108

Russ. J. Org. Chem., 2021, v. 57, No. 7, pp. 1068-1072. doi:10.1134/S107042802107006X

✔ Synthesis and certain transformations of 1,4-benzodioxane and their substituted derivatives containing 1,3,4-oxadiazole and 1,3,4-thiadiazole heterocyclic rings were carried out.

Russ. J. Org. Chem., 2020, v. 56, No. 3, pp. 385-389. doi:10.1134/S1070428020030033

Russ. J. Org. Chem., 2014, v. 50, No. 3, pp. 434-438. doi:10.1134/S1070428014030233

Russ. J. Org. Chem., 2024, v. 60, No. 9, pp. 1685-1691. doi:10.1134/S1070428024090100

Russ. J. Org. Chem., 2017, v. 53, No. 12, pp. 1905-1908. doi:10.1134/S1070428017120259

✔ The synthesis of diamide derivatives of p-aminobenzoic acid containing an arylcycloalkane and 1,4-benzodioxane fragments was developed and implemented.

Russ. J. Gen. Chem., 2015, v. 85, No. 5, pp. 1057-1062. doi:10.1134/S1070363215050096

Chem. J. Armenia, 2012, v. 65, № 2, pp. 230-238

Chem. J. Armenia, 2016, v. 69, № 1-2, pp. 111-120

Russ. J. Org. Chem., 2012, v. 48, No. 7, pp. 972-976. doi:10.1134/S1070428012070147

✔ The synthesis of new aryloxypropanolamines based on arylcyclopentane(tetrahydropyran, dimethyl)methylamines was developed and implemented

Russ. J. Org. Chem., 2016, v. 52, No. 2, pp. 209-213. doi:10.1134/S1070428016020081

Russ. J. Org. Chem., 2023, v. 59, No. 5, pp. 756-763. doi:10.1134/S1070428023050020

Russ. J. Org. Chem., 2024, v. 60, No. 1, pp. 18-24. doi:10.1134/S1070428024010032

✔ Various routes have been developed to synthesize different diamide derivatives of dibasic carboxylic acids (oxalic, succinic, and maleic).

Russ. J. Org. Chem., 2013, v. 49, No. 7, pp. 1083-1086. doi:10.1134/S1070428013070221

Chem. J. Armenia, 2012, v. 65, № 2, pp. 215-223

Chem. J. Armenia, 2012, v. 65, № 3, pp. 332-341

Chem. J. Armenia, 2013, v. 66, № 4, pp. 628-635

Chem. J. Armenia, 2012, v. 65, № 1, pp. 111-117

Russ. J. Org. Chem., 2018, v. 54, No. 6, pp. 886-891. doi:10.1134/S1070428018060106

Russ. J. Org. Chem., 2024, v. 60, No. 11, pp. 2117-2124. doi:10.1134/S1070428024110046

✔ New aryl-, 1,3-benzodioxole- and 1,4-benzodioxanylcycloalkane(tetrahydropyran)carboxylic acid aminoamide and aminoester derivatives have been developed and synthesized for the first time.

Russ. J. Gen. Chem., 2019, v. 89, No. 5, pp. 1051-1054. doi:10.1134/S107036321905027X

Russ. J. Org. Chem., 2024, v. 60, No. 6, pp. 1028-1035. doi:10.1134/S1070428024060071

Russ. J. Org. Chem., 2019, v. 55, No. 6, pp. 796-799. doi:10.1134/S1070428019060095

Russ. J. Org. Chem., 2025, v. 61, No. 3, pp. 403-411. doi:10.1134/S107042802560010X

✔ Methods for obtaining compounds with oxygen-containing heterocycles (1,4-benzodioxane, tetrahydropyran, furan) at the second position of the 1,3,4-oxadiazole ring have been developed.

Russ. J. Org. Chem., 2025, v. 61, No. 1, pp. 73-79. doi:10.1134/S1070428024602966

Russ. J. Org. Chem., 2024, v. 60, No. 4, pp. 655-663. doi:10.1134/S1070428024040146

Russ. J. Org. Chem., 2020, v. 56, No. 2, pp. 281-286. doi:10.1134/S1070428020020177

✔ Methods for the synthesis of thienopyrimidines containing fragments of 1,4-benzodioxane and phenylcyclohexanecarbonitrile have been proposed, which were carried out via the cyclization reaction of 2-amino-3-carbethoxy-substituted thiophenes.

Russ. J. Org. Chem., 2019, v. 55, No. 5, pp. 598-601. doi:10.1134/S1070428019050038

Russ. J. Org. Chem., 2022, v. 58, No. 7, pp. 977-981. doi:10.1134/S1070428022070053

Russ. J. Org. Chem., 2024, v. 60, No. 3, pp. 397-402. doi:10.1134/S1070428024030047

Russ. J. Org. Chem., 2020, v. 56, No. 3, pp. 440-445. doi:10.1134/S1070428020030124

Russ. J. Org. Chem., 2021, v. 57, No. 10, pp. 1638-1642. doi:10.1134/S1070428021100110

✔ The antihypoxic, antimonoaminoxidase, antioxidant, antiarrhythmic, anticonvulsant, and antibacterial properties of the synthesized compounds have been investigated.

The best works of recent years

Russ. J. Org. Chem., 2021, v. 57, No. 2, pp. 195-202. doi:10.1134/S1070428021020093