Literature DB >> 18240388

A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.

Dong-Mei Feng1, Robert M DiPardo, Jenny M Wai, Ronald K Chang, Christina N Di Marco, Kathy L Murphy, Richard W Ransom, Duane R Reiss, Cuyue Tang, Thomayant Prueksaritanont, Douglas J Pettibone, Mark G Bock, Scott D Kuduk.   

Abstract

The design and synthesis of a novel class of human bradykinin B1 antagonists featuring difluoroethyl ether and isoxazole carboxamide moieties are disclosed. Compound 7g displayed excellent pharmacokinetic properties, efficient ex vivo receptor occupancy, and low potential for P450 induction via PXR activation.

Entities:  

Mesh:

Substances:

Year:  2008        PMID: 18240388     DOI: 10.1016/j.bmcl.2007.11.057

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.

Authors:  Tao Liu; James P Beck; Junliang Hao
Journal:  RSC Med Chem       Date:  2022-01-19

Review 2.  Differential regulation of inducible and endothelial nitric oxide synthase by kinin B1 and B2 receptors.

Authors:  F Kuhr; J Lowry; Y Zhang; V Brovkovych; R A Skidgel
Journal:  Neuropeptides       Date:  2010-01-04       Impact factor: 3.286

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.