Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: Optimization of drug-like properties and target independent parameters

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 14, 2011, Pages 4276-4280

  Zindell, Renée ^a   Walker, Edward R ^b   Scott, John ^b   Amouzegh, Patricia ^b   Wu, Lifen ^a   Ermann, Monika ^b   Thomson, David ^a   Fisher, Micheal B ^a   Fullenwider, Cody Lee ^a   Grbic, Heather ^a   Kaplita, Paul ^a   Linehan, Brian ^a   Patel, Mita ^a   Patel, Monica ^a   Löbbe, Sabine ^c   Block, Svenja ^c   Albrecht, Claudia ^c   Gemkow, Mark J ^c   Shih, Daw Tsun ^a   Riether, Doris ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b EVOTEC UK LTD   (United Kingdom)

^c EVOTEC AG   (Germany)

Author keywords

1,4 Diazepane; Cannabinoid receptor; CB2; Drug like parameters; Permeability

Indexed keywords

BENZODIAZEPINE DERIVATIVE; BENZOXAZOLE DERIVATIVE; CANNABINOID 1 RECEPTOR AGONIST; CANNABINOID 2 RECEPTOR AGONIST; ISOXAZOLE;

ARTICLE; CONTROLLED STUDY; DRUG PENETRATION; DRUG SCREENING; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG TARGETING; HIGH THROUGHPUT SCREENING; PHARMACOLOGICAL PARAMETERS; PROCESS OPTIMIZATION;

AZEPINES; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MICROSOMES, LIVER; RECEPTOR, CANNABINOID, CB1; RECEPTOR, CANNABINOID, CB2; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79959901746     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.05.068     Document Type: Article

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