820242-67-9Relevant academic research and scientific papers
Substituted 2-phenyl-benzimidazole derivatives: novel compounds that suppress key markers of allergy
Richards, Mark L.,Lio, Shirley Cruz,Sinha, Anjana,Banie, Homayon,Thomas, Richard J.,Major, Michael,Tanji, Mark,Sircar, Jagadish C.
, p. 950 - 969 (2007/10/03)
The pharmacotherapy of allergy and asthma has traditionally focused on the effecter molecules of the allergic cascade, while neglecting targets that play an early role in their development. Reasoning that IgE is central to the expansion of atopic diseases, we identified and extended a novel family of 2-(substituted phenyl)-benzimidazole inhibitors of IgE response. Pharmacological activity depends on an intact phenylbenzimidazole-bis-amide backbone, and is optimized by the presence of lipophilic terminal groups composed of either bis cycloalkyl or combinations of aliphatic and halogen-substituted aromatic groups. These compounds also inhibit IL-4 and IL-5 responses in T cells and CD23 expression on B cells, with potencies that parallel their inhibition of IgE. The broad profile of these compounds thus underscores their potential for treating the multifarious pathology of asthma.
Novel 2-(substituted phenyl)benzimidazole derivatives with potent activity against IgE, cytokines, and CD23 for the treatment of allergy and asthma
Richards, Mark L.,Lio, Shirley Cruz,Sinha, Anjana,Tieu, Kenneth K.,Sircar, Jagadish C.
, p. 6451 - 6454 (2007/10/03)
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
