19227-14-6Relevant articles and documents
Novel O-acylated amidoximes and substituted 1,2,4-oxadiazoles synthesised from (+)-ketopinic acid possessing potent virus-inhibiting activity against phylogenetically distinct influenza A viruses
Chernyshov, Vladimir V.,Yarovaya, Olga I.,Esaulkova, Iana L.,Sinegubova, Ekaterina,Borisevich, Sophia S.,Popadyuk, Irina I.,Zarubaev, Vladimir V.,Salakhutdinov, Nariman F.
, (2021/12/16)
This article describes the synthesis and antiviral activity evaluation of new substituted 1,2,4-oxadiazoles containing a bicyclic substituent at position 5 of the heterocycle and O-acylated amidoximes as precursors for their synthesis. New compounds were
Catalyst-free, one-pot strategy to access 3-substituted-5-amino-1,2,4-thiadiazoles in water
Nagaraju, Chaithra,Ashok, Swarup Hassan,Narayana, Yatheesh,Nagarakere, Sandhya C.,Kempegowda, Mantelingu,Kanchugarkoppal, Rangappa S.
, p. 3610 - 3619 (2021/10/14)
A protocol has been devised for the synthesis of 3-substituted 5-amino-1,2,4-thiadiazoles utilizing isothiocyanates, amidoximes and water as an eco-friendly solvent. The strategy involves consecutive C?N and S?N bonds formation in a one-pot reaction under
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists
Zhang, Han,He, Xiaomeng,Wang, Xintong,Yu, Bo,Zhao, Siqi,Jiao, Peili,Jin, Hongwei,Liu, Zhenming,Wang, KeWei,Zhang, Liangren,Zhang, Lihe
, (2020/09/03)
α: 7 nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems have been suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, we started a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761–0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3 μM to 13.7 μM. Compound B10 exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The analysis of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists.