Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: Design, synthesis and structure-activity relationship studies

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 18, 2004, Pages 4607-4613

  Vergne, Fabrice ^a,b   Bernardelli, Patrick ^a   Lorthiois, Edwige ^a   Pham, Nga ^a   Proust, Emmanuelle ^a   Oliveira, Chrystelle ^a   Mafroud, Abdel Kader ^a   Royer, Frederique ^a   Wrigglesworth, Roger ^a   Schellhaas, Jennifer ^a   Barvian, Mark ^a   Moreau, François ^a   Idrissi, Moulay ^a   Tertre, Anita ^a   Bertin, Bernadette ^a   Coupe, Magali ^a   Berna, Patrick ^a   Soulard, Patricia ^a  

^a PFIZER INC   (United States)

^b SANOFI   (France)

Author keywords

camp; PDE7; Phosphodiesterase

Indexed keywords

PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE VII INHIBITOR; THIADIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CYCLIZATION; DRUG ACTIVITY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION;

3',5'-CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE; CELL LINE; HUMANS; ISOENZYMES; PHOSPHODIESTERASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES;

EID: 8544250603     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.07.008     Document Type: Article

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29. All the compounds illustrated in this report were not selective for either enzyme subtype PDE7A or PDE7B. Consequently, only PDE7A inhibitory activities are presented