Design, synthesis and biological evaluation of bisabolangelone oxime derivatives as potassium-competitive acid blockers (P-CABs)

[Display omitted] With the aim of searching novel P-CABs, seven bisabolangelone oxime derivatives were designed, synthesized, characterized and evaluated the H+,K+-ATPase inhibitory activities guided by computer aided drug design methods. The binding free energy calculations were in good agreement w...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-05, Vol.26 (9), p.2268-2272
Hauptverfasser:	Huang, Nian-Yu, Wang, Wen-Bin, Chen, Lei, Luo, Hua-Jun, Wang, Jun-Zhi, Deng, Wei-Qiao, Zou, Kun
Format:	Artikel
Sprache:	eng
Schlagworte:	Bisabolangelone Drug Design Drug Evaluation, Preclinical Drug rational design Enzyme Inhibitors - pharmacology H(+)-K(+)-Exchanging ATPase - drug effects H+,K+-ATPase inhibitory activities Oximes - chemistry P-CABs Potassium - metabolism Sesquiterpenes - chemistry Sesquiterpenes - pharmacology Synthesis
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