Novel 2-(substituted phenyl)benzimidazole derivatives with potent activity against IgE, cytokines, and CD23 for the treatment of allergy and asthma.
Novel 2-(substituted phenyl)benzimidazole derivatives with potent activity against IgE, cytokines, and CD23 for the treatment of allergy and asthma.
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DOI：
10.1021/jm049288j
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发表时间：
2004-12
影响因子：
7.3
通讯作者：
M. Richards;S. Lio;A. Sinha;K. Tieu;J. Sircar
中科院分区：
文献类型：
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作者：
M. Richards;S. Lio;A. Sinha;K. Tieu;J. Sircar
可注射抗IgE抗体omalizumab的有效性验证了IgE作为过敏性疾病的重要靶点，从而催生了小分子IgE抑制剂的开发。在这里，简要的SAR描述了新的苯并咪唑化合物，有效地抑制IgE反应。除了IgE外，这些药物还抑制其他对过敏反应至关重要的靶标。介绍了口服活性AVP-13358的概况，AVP-13358是该系列目前处于临床试验中的先导化合物。
The effectiveness of the injectable anti-IgE antibody omalizumab has validated IgE as an important target for allergic diseases, thus spawning the development of small-molecule IgE inhibitors. Herein, a brief SAR is described for novel phenylbenzimidazole compounds that potently suppress IgE responses. In addition to IgE, these agents inhibit other targets critical for allergic response. The profile of orally active AVP-13358, the lead compound of this series currently in clinical trials, is described.