Bioorganic & Medicinal Chemistry Letters 2010-10-01

Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.

Wilna J Moree, Bin-Feng Li, Said Zamani-Kord, Jinghua Yu, Timothy Coon, Charles Huang, Dragan Marinkovic, Fabio C Tucci, Siobhan Malany, Margaret J Bradbury, Lisa M Hernandez, Jianyun Wen, Hua Wang, Samuel R J Hoare, Robert E Petroski, Kayvon Jalali, Chun Yang, Aida Sacaan, Ajay Madan, Paul D Crowe, Graham Beaton

文献索引：Bioorg. Med. Chem. Lett. 20(19) , 5874-8, (2010)

全文：HTML全文

摘要

Analogs of the known H(1)-antihistamine R-dimethindene with suitable selectivity for key GPCRs, P450 enzymes and hERG channel were assessed for metabolism profile and in vivo properties. Several analogs were determined to exhibit diverse metabolism. One of these compounds, 10a, showed equivalent efficacy in a rat EEG/EMG model to a previously identified clinical candidate and a potentially superior pharmacokinetic profile as determined from a human microdose study.Copyright © 2010 Elsevier Ltd. All rights reserved.

相关化合物

  • 茚
  • 马来酸二甲茚定

相关文献：

Fibronectin enhances spinal cord astrocyte proliferation by elevating P2Y1 receptor expression.

2014-08-01

[J. Neurosci. Res. 92(8) , 1078-90, (2014)]

Decoys for docking.

2005-06-02

[J. Med. Chem. 48 , 3714-28, (2005)]

One pot synthesis of indene through copper(I)-catalyzed three-components coupling and cyclization reaction.

2012-05-14

[Org. Biomol. Chem. 10(18) , 3636-41, (2012)]

Exciton dissociation and charge-transport enhancement in organic solar cells with quantum-dot/N-doped CNT hybrid nanomaterials.

2013-04-11

[Adv. Mater. 25(14) , 2011-7, (2013)]

Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.

2007-04-19

[J. Med. Chem. 50 , 1876-85, (2007)]

更多文献...