Derivatives of a new heterocyclic system – pyrano[3, 4-c][1, 2, 4]triazolo[4, 3-a]pyridines: synthesis, docking analysis and neurotropic activity. Issue 8 (19th June 2019)

• Record Type: Journal Article
• Authors: Paronikyan, Ervand G.; Petrou, Anthi; Fesatidou, Maria; Geronikaki, Athina; Dashyan, Shushanik Sh.; Mamyan, Suren S.; Paronikyan, Ruzanna G.; Nazaryan, Ivetta M.; Hakopyan, Hasmik H.
• Is Part Of: MedChemComm. Volume 10:Issue 8(2019)
• Page Start: 1399
• Page End: 1411
• Publication Date: 2019-06-19
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c9md00187e
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : 8-Hydrazino derivatives of pyrano[3, 4- c ]pyridines and derivatives of new heterocyclic system 3-thioxopyrano[3, 4- c ][1, 2, 4]triazolo[4, 3- a ]pyridines were synthesized and evaluated for their neurotropic activity. The most active compound in all tests appeared to be5g . Abstract : 8-Hydrazino derivatives of pyrano[3, 4- c ]pyridines and derivatives of the new heterocyclic system 3-thioxopyrano[3, 4- c ][1, 2, 4]triazolo[4, 3- a ]pyridines on the basis of methanesulfonates of pyrano[3, 4- c ]pyridinium were synthesized by optimization of a previously used method. Derivatives of alkylsulfonyl pyrano[3, 4- c ][1, 2, 4]triazolo[4, 3- a ]pyridines were also synthesized. All compounds were evaluated for their neurotropic activity. Among all the compounds tested for anticonvulsant activity by pentylenetetrazole and maximal electric shock seizure (MES) tests, six compounds (5a, 5b, 5e, 5g, 5j, and5p ) appeared to be active. These compounds were also evaluated for their anxiolytic as well as antidepressant activities using "open field", "elevated plus maze" (EPM), and "forced swimming" tests, respectively. It should be mentioned that compounds tested by the "rotating rod" method did not affect neuromuscular coordination. The most active compound appeared to be5g in all tests. Docking studies of the most active compounds were performed on the GABAA receptor, SERT and 5-HT1A receptor.