Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 8, 2008, Pages 2544-2548

  Barbay, J Kent ^a   Gong, Yong ^a   Buntinx, Mieke ^b   Li, Jian ^a   Claes, Concha ^b   Hornby, Pamela J ^a   Van Lommen, Guy ^b   Van Wauwe, Jean ^b   He, Wei ^a  

^a Drug Discovery   (United States)

^b Oncology Drug Discovery   (Belgium)

Author keywords

C5a; C5a receptor antagonist; C5aR; Complement; Tetrahydroquinoline

Indexed keywords

COMPLEMENT COMPONENT C5 INHIBITOR;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CROSS COUPLING REACTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; LIVER MICROSOME; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

AMINES; HUMANS; MICROSOMES, LIVER; MOLECULAR STRUCTURE; QUINOLINES; RECEPTOR, ANAPHYLATOXIN C5A; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 41949133045     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.03.049     Document Type: Article

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24. All compounds shown in Table 3 were prepared by the route depicted in Scheme 2a. Except as specifically noted in the text, all other compounds were prepared using the route of Scheme 1.
25. 50 values were calculated using non-linear regression in Graphpad Prism.
26. i values were calculated using the equation of Cheng and Prusoff (Biochem. Pharmacol. 1973, 22, 3099) in Graphpad Prism.