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苯并咪唑类作为治疗过敏性鼻炎的新型强效选择性DP拮抗剂。

Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.

作者信息

Beaulieu Christian, Wang Zhaoyin, Denis Danielle, Greig Gillian, Lamontagne Sonia, O'Neill Gary, Slipetz Deborah, Wang Jennifer

机构信息

Merck Frosst Centre for Therapeutic Research, PO Box 1005, Kirkland, QC, Canada H9R 4P8.

出版信息

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3195-9. doi: 10.1016/j.bmcl.2004.04.005.

Abstract

A series of 2-substituted N-benzyl benzimidazole containing molecules has been synthesized and its structure-activity relationship for the human DP receptor has been evaluated. Selective DP antagonists with nanomolar potency for the DP receptor were identified in this novel series of benzimidazoles.

摘要

已合成了一系列含2-取代N-苄基苯并咪唑的分子,并评估了其对人DP受体的构效关系。在这一系列新型苯并咪唑中鉴定出了对DP受体具有纳摩尔效力的选择性DP拮抗剂。

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