Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: Metabolism-directed optimization studies towards orally bioavailable derivatives

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 18, 2004, Pages 4615-4621

  Vergne, Fabrice ^a,b   Bernardelli, Patrick ^a   Lorthiois, Edwige ^a   Pham, Nga ^a   Proust, Emmanuelle ^a   Oliveira, Chrystelle ^a   Mafroud, Abdel Kader ^a   Ducrot, Pierre ^a   Wrigglesworth, Roger ^a   Berlioz Seux, Françoise ^a   Coleon, Francis ^a   Chevalier, Eric ^a   Moreau, François ^a   Idrissi, Moulay ^a   Tertre, Anita ^a   Descours, Arnaud ^a   Berna, Patrick ^a   Li, Mei ^a  

^a PFIZER INC   (United States)

^b SANOFI   (France)

Author keywords

ADME; cAMP; PDE7; Phosphodiesterase

Indexed keywords

PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE VII; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG METABOLISM; DRUG SELECTIVITY;

3',5'-CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE; ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; ISOENZYMES; PHOSPHODIESTERASE INHIBITORS; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES;

EID: 8544256308     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.07.009     Document Type: Article

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