Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics was written by Shi, Wenqiang;Wang, Yu;Wu, Chunhui;Yang, Feipu;Zheng, Wei;Wu, Song;Liu, Yongjian;Wang, Zhen;He, Yang;Shen, Jingshan. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Category: pyridine-derivatives This article mentions the following:
A series of triazolopyridinone derivatives originating from the antidepressant trazodone was designed and pharmacol. evaluated. Most of the compounds with a multireceptor functional profile exhibited high potency at the D2, 5-HT1A, and 5-HT2A receptors. Compounds 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2 H)-one, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-8-fluoro-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-5-methoxy-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one and 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3-oxo-2,3-dihydro-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrile were selected for further evaluation of druggable potential. Among these compounds, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one, as a D2 receptor partial agonist, demonstrated very potent inhibition of quipazine-induced head-twitch response, which validated its 5-HT2A receptor antagonistic efficacy in vivo. 2-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2-H)-one also demonstrated a dose-dependent effect on PCP-induced hyperactivity when administered orally. Thus, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one endowed with a triazolopyridinone scaffold represents a valuable lead for the development of novel atypical antipsychotics. In the experiment, the researchers used many compounds, for example, 6-Fluoronicotinonitrile (cas: 3939-12-6Category: pyridine-derivatives).
6-Fluoronicotinonitrile (cas: 3939-12-6) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Category: pyridine-derivatives