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ID: ALA1139432

Journal: Bioorg Med Chem Lett

Title: Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.

Authors: Biswas K, Aya T, Qian W, Peterkin TA, Chen JJ, Human J, Hungate RW, Kumar G, Arik L, Lester-Zeiner D, Biddlecome G, Manning BH, Sun H, Dong H, Huang M, Loeloff R, Johnson EJ, Askew BC.

Abstract: We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models.

CiteXplore: 18706809

DOI: 10.1016/j.bmcl.2008.07.108