851179-06-1Relevant articles and documents
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics
Shi, Wenqiang,Wang, Yu,Wu, Chunhui,Yang, Feipu,Zheng, Wei,Wu, Song,Liu, Yongjian,Wang, Zhen,He, Yang,Shen, Jingshan
, (2020)
A series of triazolopyridinone derivatives originating from the antidepressant trazodone was designed and pharmacologically evaluated. Most of the compounds with a multireceptor functional profile exhibited high potency at the D2, 5-HT1A, and 5-HT2A receptors. Compounds S1, S3, S9 and S12 were selected for further evaluation of druggable potential. Among these compounds, S1, 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. S1 also demonstrated a dose-dependent effect on PCP-induced hyperactivity when administered orally. Thus, S1 endowed with a triazolopyridinone scaffold represents a valuable lead for the development of novel atypical antipsychotics.
A O-carboxamide benzamide derivatives, preparation method thereof and a pesticide (by machine translation)
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Paragraph 0086, (2017/08/25)
The present invention provides a kind of formula (I) the structure shown as the O-carboxamide benzamide derivatives. In order to its preparation of insecticide, agricultural, forestry and other common pest with broad-spectrum, high activity, long lasting period and the like, in addition to preventing bollworm, Diamondback moth, Lepidoptera beet pest have very good effect the outer, thereof for the aphid and Homoptera pest also having very good application prospects, therefore in the pest control in the process, can be used as active ingredients used alone, without the need for other insecticides. (by machine translation)
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors
Aiguadé, Josep,Balagué, Cristina,Carranco, Inés,Caturla, Francisco,Domínguez, María,Eastwood, Paul,Esteve, Cristina,González, Jacob,Lumeras, Wenceslao,Orellana, Adelina,Preciado, Sara,Roca, Ramón,Vidal, Laura,Vidal, Bernat
experimental part, p. 3431 - 3436 (2012/06/18)
A new class of p38α inhibitors based on a biaryl-triazolopyridine scaffold was investigated. X-ray crystallographic data of the initial lead compound cocrystallised with p38α was crucial in order to uncover a unique binding mode of the inhibitor to the hinge region via a pair of water molecules. Synthesis and SAR was directed towards the improvement of binding affinity, as well as ADME properties for this new class of p38α inhibitors and ultimately afforded compounds showing good in vivo efficacy.