Substituted 2-phenyl-benzimidazole derivatives: novel compounds that suppress key markers of allergy

European Journal of Medicinal Chemistry
Mark L RichardsJagadish C Sircar

Abstract

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.

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Citations

Aug 11, 2007·Cancer Chemotherapy and Pharmacology·Shirley Cruz LioMark L Richards
Feb 26, 2013·Chemical Reviews·Lukas WankaPeter R Schreiner
Sep 29, 2011·Acta Pharmaceutica : a Quarterly Journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, Dealing with All Branches of Pharmacy and Allied Sciences·Ramesh Sawant, Deepali Kawade
Feb 3, 2018·Organic & Biomolecular Chemistry·Saurabh SharmaPralay Das
Jun 13, 2008·Journal of Combinatorial Chemistry·Hee-Jong LimMyung Hee Jung
Nov 2, 2007·Journal of Medicinal Chemistry·Homayon BanieMark L Richards

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