Synthesis and evaluation of novel prodrugs of caspase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 485-488

  Charrier, Jean Damien ^a   Durrant, Steven J ^a   Studley, John ^a   Lawes, Linda ^a   Weber, Peter ^a  

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

6,6a Dihydrofuro 3,2 d oxazol 5(3aH) one; Caspase inhibitor; Ketalisation cyclodehydration; Oral availability; Prodrug

Indexed keywords

CASPASE INHIBITOR; EMRICASAN; FURO[3,2 D]OXAZOLE; NIVOCASAN; PRALNACASAN; PRODRUG; UNCLASSIFIED DRUG; VRT 18858; VX 166;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DIASTEREOISOMER; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EXPOSURE; DRUG SCREENING; DRUG STABILITY; DRUG SYNTHESIS; HUMAN; IN VITRO STUDY; LIPOPHILICITY; NONHUMAN; RAT; SYSTEMIC CIRCULATION;

ADMINISTRATION, ORAL; ANIMALS; APOPTOSIS; AREA UNDER CURVE; CASPASE 1; CELL LINE; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; HYDROLYSIS; MODELS, CHEMICAL; MOLECULAR CONFORMATION; PEPTIDES; PEPTIDOMIMETICS; PRODRUGS; RATS; STEREOISOMERISM;

RATTUS;

EID: 84655163500     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.102     Document Type: Article

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