Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 14, 2008, Pages 3852-3855

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

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

Aniline; Antagonist; C5aR; Complement C5a; Tetrahydroquinoline

Indexed keywords

ANILINE DERIVATIVE; COMPLEMENT COMPONENT C5A RECEPTOR; COMPLEMENT COMPONENT C5A RECEPTOR BLOCKING AGENT; COMPLEMENT INHIBITOR; ECULIZUMAB; QUINOLINE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; CALCIUM MOBILIZATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANILINE COMPOUNDS; BINDING SITES; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; LIGANDS; MODELS, CHEMICAL; MOLECULAR CONFORMATION; MOLECULAR STRUCTURE; QUINOLINES; RECEPTOR, ANAPHYLATOXIN C5A; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 47149108682     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.06.059     Document Type: Article

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19. 2O: C, 76.50; H, 8.03; N, 6.37. Found: C, 76.48; H, 7.96; N, 6.16.
20. The plasma level of 27, a potential des-methyl metabolite, was also found to be minimal.