19533-08-5Relevant articles and documents
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities
Li, Feng,Xu, Qinlong,Zhu, Qihua,Chu, Zhaoxing,Lin, Gaofeng,Mo, Jiajia,Zhao, Yan,Li, Jiaming,He, Guangwei,Xu, Yungen
, (2019/11/03)
To improve the anti-inflammatory activity of desloratadine, we designed and synthesized a series of novel desloratadine derivatives. All compounds were evaluated for their anti-inflammatory and H1 antagonistic activities. Among them, compound 2c showed the strongest H1 antagonistic and anti-inflammatory activity. It also exhibited promising pharmacokinetic profiles and low toxicity. All these results suggest that compound 2c as a novel anti-allergic agent is worthy of further investigation.
The hERG potassium channel and drug trapping: Insight from docking studies with propafenone derivatives
Thai, Khac-Minh,Windisch, Andreas,Stork, Daniela,Weinzinger, Anna,Schiesaro, Andrea,Guy, Robert H.,Timin, Eugen N.,Hering, Steffen,Ecker, Gerhard F.
scheme or table, p. 436 - 442 (2010/11/17)
The inner cavity of the hERG potassium ion channel can accommodate large, structurally diverse compounds that can be trapped in the channel by closure of the activation gate. A small set of propafenone derivatives was synthesized, and both use-dependency and recovery from block were tested in order to gain insight into the behavior of these compounds with respect to trapping and non-trapping. Ligand-protein docking into homology models of the closed and open state of the hERG channel provides the first evidence for the molecular basis of drug trapping.
Synthesis and pharmacological evaluation of some potential beta-adrenolytics derivated from o-hydroxyacetophenone
Cizmarikova,Racanska,Dingova,Greksakova
, p. 366 - 367 (2007/10/02)
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