Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 17, 2005, Pages 3925-3929

  Kuduk, Scott D ^a   Chang, Ronald K ^a   Ng, Christina ^a   Murphy, Kathy L ^a   Ransom, Richard W ^a   Tang, Cuyue ^b   Prueksaritanont, Thomayant ^b   Freidinger, Roger M ^a   Pettibone, Douglas J ^a   Bock, Mark G ^a  

^a Department of Medicinal Chemistry ^*  (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Bradykinin; Diaminopyridine

Indexed keywords

AMINOPYRIDINE DERIVATIVE; BRADYKININ B1 RECEPTOR ANTAGONIST; PIPERIDINE; 2,3 DIAMINOPYRIDINE; 2,3-DIAMINOPYRIDINE; BRADYKININ; BRADYKININ B1 RECEPTOR;

ARTICLE; DRUG BIOAVAILABILITY; DRUG POTENCY; NONHUMAN; RAT; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; ANIMAL; DRUG ANTAGONISM; HUMAN; PHARMACOKINETICS; PROTEIN BINDING; SPRAGUE DAWLEY RAT; SYNTHESIS;

AMINOPYRIDINES; ANIMALS; BRADYKININ; HUMANS; PHARMACOKINETICS; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, BRADYKININ B1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 23244449648     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.05.133     Document Type: Article

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12. The olefin in the C-ring of 14a was later reduced to the cyclohexane derivative (Raney Nickel) after the pyridine was attached to give 14b as shown in Scheme 1.