Bioorganic & Medicinal Chemistry Letters 2005-05-02

2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.

Dong-Mei Feng, Jenny M Wai, Scott D Kuduk, Christina Ng, Kathy L Murphy, Richard W Ransom, Duane Reiss, Raymond S L Chang, Charles M Harrell, Tanya MacNeil, Cuyue Tang, Thomayant Prueksaritanont, Roger M Freidinger, Douglas J Pettibone, Mark G Bock

Index: Bioorg. Med. Chem. Lett. 15(9) , 2385-8, (2005)

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Abstract

A novel class of 2,3-diaminopyridine bradykinin B1 receptor antagonists is disclosed. Structure-activity relationship studies (SARs) that led to compounds with significantly improved potency and pharmacokinetic properties relative to the lead compound are described.