41841-19-4Relevant articles and documents
Discovery, synthesis, and structure-activity relations of 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-ones as potassium-competitive acid blockers
Imaeda, Toshihiro,Ono, Koji,Nakai, Kazuo,Hori, Yasunobu,Matsukawa, Jun,Takagi, Terufumi,Fujioka, Yasushi,Tarui, Naoki,Kondo, Mitsuyo,Imanishi, Akio,Inatomi, Nobuhiro,Kajino, Masahiro,Itoh, Fumio,Nishida, Haruyuki
, p. 3719 - 3735 (2017/06/13)
With the aim to discover a gastric antisecretory agent more potent than the existing proton pump inhibitors, novel 3,4-dihydro-1H-spiro(naphthalene-2,2′-piperidin)-1-one derivatives, which could occupy two important lipophilic pockets (described as LP-1 and LP-2) of H+,K+-ATPase and can strongly bind to the K+-binding site, were designed based on a docking model. Among the compounds synthesized, compound 4d showed a strong H+,K+-ATPase-inhibitory activity and a high stomach concentration in rats, resulting in potent inhibitory action on histamine-stimulated gastric acid secretion in rats. Furthermore, 4d exerted significant inhibitory action on histamine-stimulated gastric-acid secretion in rats with a rapid onset and moderate duration of action after the administration. These findings may lead to a new insight into the drug design of potassium-competitive acid blockers.
NOVEL BETA MIMETICS WITH EXTENDED DURATION OF ACTION, METHOD FOR PRODUCTION AND USE THEREOF AS MEDICAMENTS
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Page/Page column 9, (2010/02/06)
The invention relates to compounds of general formula (I), where the groups R1, R2 and R3 can have the meanings given in the claims and the description, method for production and use thereof as medicaments, in particular for the treatment of inflammatory and obstructive bronchial diseases.
Unusual Kinetic Stability of Enols to Ketonization: 1,2-Dimesityl-3-methylbut-1-en-1-ol and Related β-Alkyl-α,β-dimesitylethenols
Nadler, Ella B.,Rappoport, Zvi
, p. 2673 - 2682 (2007/10/02)
The β-alkyl-α,β-dimesitylethenols 3 and the isomeric β-alkyl-α,β-dimesitylethanones 4 (β-alkyl = Me, Et, i-Pr) were prepared and their spectral properties are reported.X-ray diffraction of the β-isopropyl enol 3d showed that the two mesityl rings are near