Synthesis and pharmacological investigation of azaphthalazinone human histamine H1 receptor antagonists

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 20, 2012, Pages 6097-6108

  Procopiou, Panayiotis A ^a   Browning, Christopher ^a   Gore, Paul M ^a   Lynn, Sean M ^a   Richards, Stephen A ^a   Slack, Robert J ^a   Sollis, Steven L ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Allergic rhinitis; H1 receptor antagonist; Phthalazinone; SAR

Indexed keywords

1 [(4 CHLOROPHENYL)METHYL] 3 [2 PYRROLIDINYLMETHYL]PYRIDO[3,4 D]PYRIDAZIN 4(3H) ONE; 1 [(4 CHLOROPHENYL)METHYL] 3 [[1 METHYL 2 PYRROLIDINYL]METHYL]PYRIDO[3,4 D]PYRIDAZIN 4(3H) ONE; 11 [(4 CHLOROPHENYL)METHYL]PYRIDO[3,4 D]PYRIDAZIN 4(3H) ONE; 2 [(ETHYLOXY)CARBONYL] 3 PYRIDINECARBOXYLIC ACID; 2 [2 (4 CHLOROPHENYL) 3 (METHYLOXY) 3 OXOPROPANOYL] 2 PYRIDINECARBOXYLIC ACID; 2 [[1 BUTYL 2 PYRROLIDINYL]METHYL] 4 [(4 CHLOROPHENYL)METHYL] 1 (2H) PHTHALAZINONE; 2 [[1 BUTYL 2 PYRROLIDINYL]METHYL] 4 [(4 CHLOROPHENYL)METHYL]PYRIDO[3,4 D]PYRIDAZIN 1(2H) ONE FORMIC ACID; 4 [(4 CHLOROPHENYL)METHYL] 2 [2 PYRROLIDINYLMETHYL]PYRIDO[3,4 D]PYRIDAZIN 1(2H) ONE; 4 [(4 CHLOROPHENYL)METHYL] 2 [[1 [2 (METHYLOXY)ETHYL] 2 PYRROLIDINYL]METHYL] 1(2H) PHTHALAZINONE TRIFLUOROACETIC ACID; 4 [(4 CHLOROPHENYL)METHYL] 2 [[1 [2 (METHYLOXY)ETHYL] 2 PYRROLIDINYL]METHYL]PYRIDO[3,4 D]PYRIDAZIN 4(3H) ONE; 4 [(4 CHLOROPHENYL)METHYL] 2 [[1 [4 [4 [[3 (HEXAHYDRO 1H AZEPIN 1 YL)PROPYL]OXY]PHENYL]BUTYL] 2 PYRROLIDINYL]METHYL]PYRIDO[3,4 D]PYRIDAZIN 1(2H) ONE; 4 [(4 CHLOROPHENYL)METHYL] 2 [[1 METHYL 2 PYRROLIDINYL]METHYL]PYRIDO[3,4 D]PYRIDAZIN 1(2H) ONE; 4 [(4 CHLOROPHENYL)METHYL]PYRIDO[3,4 D]PYRIDAZIN 1(2H) ONE; 4 [(METHYLOXY)CARBONYL] 3 PYRIDINECARBOXYLIC ACID; 5 [(4 CHLOROPHENYL)METHYL] 7 [[1 METHYL 2 PYRROLIDINYL]METHYL]PYRIDO[2,3 D]PYRIDAZIN 8(7H) ONE FORMIC ACID; 5,8 DIAZAPHTHALAZINONE; 6 [[1 BUTYL 2 PYRROLIDINYL]METHYL] 8 [(4 CHLOROPHENYL)METHYL]PYRIDO[2,3 D]PYRIDAZIN 8(7H) ONE; 7 [[1 BUTYL 2 PYRROLIDINYL]METHYL] 5 [(4 CHLOROPHENYL)METHYL]PYRIDO[2,3 D]PYRIDAZIN 8(7H) ONE TRIFLUOROACETIC ACID; 8 [(4 CHLOROPHENYL)METHYL] 6 [[1 METHYL 2 PYRROLIDINYL]METHYL]PYRAZINO[2,3 D]PYRIDAZIN 5(6H) ONE; 8 [(4 CHLOROPHENYL)METHYL] 6 [[1 METHYL 2 PYRROLIDINYL]METHYL]PYRIDO[2,3 D]PYRIDAZIN 5(6H) ONE; AZAPHTHALAZINONE DERIVATIVE; AZELASTINE; ETHYL 3 [2 (4 CHLOROPHENYL) 3 (METHYLOXY) 3 OXOPROPANOYL] 2 PYRIDINECARBOXYLIC ACID; HISTAMINE H1 RECEPTOR; HISTAMINE H1 RECEPTOR ANTAGONIST; HISTAMINE H3 RECEPTOR ANTAGONIST; METHYL 3 [(4 CHLOROPHENYL)ACETYL] 4 PYRIDINECARBOXYLIC ACID; METHYL 3 [2 (4 CHLOROPHENYL) 3 [(1,1 DIMETHYLETHYL)OXY] 3 OXOPROPANOYL] 4 PYRIDINECARBOXYLIC ACID; PHTHALAZINONE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ALKYLATION; ALLERGIC RHINITIS; ARTICLE; BINDING AFFINITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DECARBOXYLATION; DEPROTECTION REACTION; DRUG ACTIVATION; DRUG HYDROLYSIS; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; HYDROPHILICITY; IN VITRO STUDY; LIPOPHILICITY; MITSUNOBU REACTION; RECEPTOR AFFINITY; RECEPTOR BLOCKING; STEREOCHEMISTRY;

ETHER-A-GO-GO POTASSIUM CHANNELS; HISTAMINE H1 ANTAGONISTS; HUMANS; PHTHALAZINES; PROTEIN BINDING; PYRAZINES; PYRIDAZINES; PYRIDINES; RECEPTORS, HISTAMINE H1; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84866929270     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.08.032     Document Type: Article

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