Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 2, 2015, Pages 322-326

  Han, Sangdon ^a   Thoresen, Lars ^a   Zhu, Xiuwen ^a   Narayanan, Sanju ^a   Jung, Jae Kyu ^a   Strah Pleynet, Sonja ^a   Decaire, Marc ^a   Choi, Karoline ^a   Xiong, Yifeng ^a   Yue, Dawei ^a   Semple, Graeme ^a   Thatte, Jayant ^a   Solomon, Michelle ^a   Fu, Lixia ^a   Whelan, Kevin ^a   Al Shamma, Hussien ^a   Gatlin, Joel ^a   Chen, Ruoping ^a   Dang, Huong ^a   Pride, Cameron ^a   Gaidarov, Ibragim ^a   Unett, David J ^a   Behan, Dominic P ^a   Sadeque, Abu ^a   Usmani, Khawja A ^a   Chen, Chuan ^a   Edwards, Jeffrey ^a   Morgan, Michael ^a   Jones, Robert M ^a   more..

^a ARENA PHARMACEUTICALS   (United States)

Author keywords

2 receptor; agonist; Cannabinoid; CB2; Pain

Indexed keywords

1 (2,4 DICHLOROPHENYL) 5 (4 IODOPHENYL) 4 METHYL N (1 PIPERIDYL) 1H PYRAZOLE 3 CARBOXAMIDE; 1ALPHA,2,5,5ALPHA TETRAHYDRO 1H 2,3 DIAZA CYCLOPROPA[A]PENTALEN 4 CARBOXAMIDE DERIVATIVE; AMIDE; ANALGESIC AGENT; CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR AGONIST; LIGAND; UNCLASSIFIED DRUG; CANNABINOID 2 RECEPTOR; FUSED HETEROCYCLIC RINGS; PYRAZOLE DERIVATIVE;

ANALGESIC ACTIVITY; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DEVELOPMENT; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VIVO STUDY; INFLAMMATORY PAIN; LOCOMOTION; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; OSTEOARTHRITIS; RAT; STRUCTURE ACTIVITY RELATION; VOLUME OF DISTRIBUTION AT STEADY-STATE; AGONISTS; ANIMAL; ARTHRITIS, EXPERIMENTAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; INFLAMMATION; LIVER MICROSOME; METABOLISM; ORAL DRUG ADMINISTRATION; PAIN; RADIOASSAY; SPRAGUE DAWLEY RAT; STEREOISOMERISM;

RODENTIA;

ADMINISTRATION, ORAL; ANALGESICS, NON-NARCOTIC; ANIMALS; ARTHRITIS, EXPERIMENTAL; HETEROCYCLIC COMPOUNDS, 3-RING; HUMANS; INFLAMMATION; MALE; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; OSTEOARTHRITIS; PAIN; PYRAZOLES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, CANNABINOID, CB1; RECEPTOR, CANNABINOID, CB2; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84922295576     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.11.040     Document Type: Article

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