4237-73-4Relevant articles and documents
8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study
Xing, Gang,Zhi, Zhengxing,Yi, Ce,Zou, Jitian,Jing, Xuefeng,Yiu-Ho Woo, Anthony,Lin, Bin,Pan, Li,Zhang, Yuyang,Cheng, Maosheng
, (2021/07/19)
β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 2-agonists among the compounds tested. They behaved as partial β2-agonists in non-overexpressed HEK293 cells, and possessed rapid smooth muscle relaxant actions and long duration of action in isolated guinea pig tracheal strip preparations. In summary, B05 and C08 are β2-agonists with potential applicability in chronic respiratory diseases.
An improved preparation of a tertiary alcohol proline linker and its use in a synthesis of mosquito oostatic hormone
Kochansky,Wagner
, p. 8007 - 8010 (2007/10/02)
An improved synthesis of 4-(3'-hydroxy-3'-methylbutyl)phenoxyacetic acid was developed using THF to overcome solubility problems initially encountered in trying to reproduce the published preparation. This hydroxyacid linker was coupled to aminomethyl polystyrene resin and used for a synthesis of the mosquito oostatic hormone by the Fmoc protocol. Attempts to prepare this insect peptide by other techniques had failed because of loss of cyclo-Pro2 from the resin.
Synthesis of 3-Hydroxy-2,3,4,5-tetrahydro-3-methylbenzoxepins by Ring-closure of Isoprenyl Terminal Epoxides
Baird, Kenneth J.,Grundon, Michael F.
, p. 1820 - 1825 (2007/10/02)
Terminal olefins (13), obtained from reactions of tertiary chlorides (10) with triphenylmethyl-lithium, were converted into epoxides (14); base-induced ring-closure of the latter gave 2-hydroxymethyl-2-methylchromans (15) and 3-hydroxy-2,3,4,5-tetrahydro-3-methylbenzoxepins (17).Dehydration of the tetrahydrobenzoxepin (17a) furnished dihydrobenzoxepins.