Samvel N Sirakanyan, Domenico Spinelli, Athina Geronikaki, Elmira K Hakobyan, Anti Petrou, Victor G Kartsev, Hasmik A Yegoryan, Ervand G Paronikyan, Luca Zuppiroli, Hasmik V Jughetsyan, Ruzanna G Paronikyan, Tatevik A Arakelyan, Anush A Hovakimyan
Author Information
Samvel N Sirakanyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru. ORCID
Domenico Spinelli: Dipartimento di Chimica G. Ciamician, Alma Mater Studiorum-Universit�� di Bologna Via F. Selmi 2 Bologna 40126 Italy domenico.spinelli@unibo.it.
Athina Geronikaki: Aristotle University of Thessaloniki, School of Pharmacy Thessaloniki-54124 Greece geronik@pharm.auth.gr.
Elmira K Hakobyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Anti Petrou: Aristotle University of Thessaloniki, School of Pharmacy Thessaloniki-54124 Greece geronik@pharm.auth.gr.
Victor G Kartsev: InterBioScreen Moscow 119019 Russia vkartsev@ibscreen.chg.ru.
Hasmik A Yegoryan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Ervand G Paronikyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Luca Zuppiroli: Department of Industrial Chemistry 'Toso Montanari', Alma Mater Studiorum-Universit�� di Bologna Viale del Risorgimento 4 Bologna 40136 Italy luca.zuppiroli@unibo.it.
Hasmik V Jughetsyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Ruzanna G Paronikyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Tatevik A Arakelyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Anush A Hovakimyan: Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L. Mnjoyan 0014 Armenia shnnr@mail.ru.
Herein, we describe the synthesis of new hybrids linked to 1,2,3- and 1,2,4-triazole units. Hybrids connected to a 1,2,3-triazole ring were synthesized using the well-known click reaction. The synthesis of the 1,2,4-triazole-based hybrids was carried out using 2-[(4-cyano-1-methyl(2-furyl)-5,6,7,8-tetrahydroisoquinolin-3-yl)oxy]acetohydrazides as starting compounds. The compounds were evaluated for their anticonvulsive activity antagonism towards pentylenetetrazole (PTZ) - and thiosemicarbazide (TSC)-induced convulsion and maximal electroshock-induced seizure (MES). Furthermore, the most active compounds were studied for their locomotory and anxiolytic activity the "open field" and elevated plus maze (EPM) assays. Finally, their antidepressant activity was studied the "forced swim" method. All the hybrids displayed pentylenetetrazole antagonism, ranging from 40% to 80%, while in the TSC model, the most active compounds increased latency of thiosemicarbazide seizures to 1.9-4.65 times compared to that of the control. Some of the tested compounds exhibited a pronounced anxiolytic and antidepressant effect. Docking study demonstrated complete agreement with experimental pharmacological data. It was revealed that the most active compounds have a pyrano[3,4-]pyridine ring in their structure.
