Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 3, 2015, Pages 581-586

  Riether, Doris ^b   Zindell, Renee ^a   Wu, Lifen ^a   Betageri, Raj ^a   Jenkins, James E ^c   Khor, Someina ^c   Berry, Angela K ^a   Hickey, Eugene R ^a   Ermann, Monika ^c   Albrecht, Claudia ^d   Ceci, Angelo ^b   Gemkow, Mark J ^d   Nagaraja, Nelamangala V ^a   Romig, Helmut ^b   Sauer, Achim ^b   Thomson, David S ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

^c EVOTEC UK LTD   (United Kingdom)

^d EVOTEC AG   (Germany)

Author keywords

Cannabinoid receptor 2 (CB2); Metabolic stability; Pharmacokinetic properties; Proline; Solubility

Indexed keywords

4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; CANNABINOID 2 RECEPTOR; CANNABINOID 2 RECEPTOR AGONIST; DULOXETINE; STREPTOZOCIN; CANNABINOID 1 RECEPTOR; ISOXAZOLE DERIVATIVE; LIGAND; PROLINE; PROTEIN BINDING; PYROGLUTAMIC ACID;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CAMP ASSAY; CHO CELL LINE; CONTROLLED STUDY; CROSS REACTION; DOSE RESPONSE; DRUG BINDING; DRUG BINDING SITE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG PENETRATION; DRUG RECEPTOR BINDING; DRUG SOLUBILITY; DRUG STABILITY; EC50; FEMALE; HUMAN; HYPERALGESIA; IC50; LIVER MICROSOME; NEUROPATHIC PAIN; NONHUMAN; POINT MUTATION; PROCESS OPTIMIZATION; RAT; SEDATION; STREPTOZOTOCIN-INDUCED DIABETIC NEUROPATHY; STRUCTURE ACTIVITY RELATION; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; CHEMICALLY INDUCED; CHEMISTRY; DIABETIC NEUROPATHIES; HALF LIFE TIME; MALE; METABOLISM; SOLUBILITY; WISTAR RAT;

ANIMALS; DIABETIC NEUROPATHIES; HALF-LIFE; HUMANS; ISOXAZOLES; LIGANDS; MALE; MICROSOMES, LIVER; PROLINE; PROTEIN BINDING; PYRROLIDONECARBOXYLIC ACID; RATS; RATS, WISTAR; RECEPTOR, CANNABINOID, CB1; RECEPTOR, CANNABINOID, CB2; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84920780630     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.12.019     Document Type: Article

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