Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.844-849
- Wu, Wen-Lian
- Asberom, Theodros
- Bara, Thomas
- Bennett, Chad
- Burnett, Duane A.
- Clader, John
- Domalski, Martin
- Greenlee, William J.
- Josien, Hubert
- McBriar, Mark
- Rajagopalan, Murali
- Vicarel, Monica
- Xu, Ruo
- Hyde, Lynn A.
- Del Vecchio, Robert A.
- Cohen-Williams, Mary E.
- Song, Lixin
- Lee, Julie
- Terracina, Giuseppe
- Zhang, Qi
- Nomeir, Amin
- Parker, Eric M.
- Zhang, Lili
2013
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- Autor(en) / Beteiligte
- Wu, Wen-Lian
- Asberom, Theodros
- Bara, Thomas
- Bennett, Chad
- Burnett, Duane A.
- Clader, John
- Domalski, Martin
- Greenlee, William J.
- Josien, Hubert
- McBriar, Mark
- Rajagopalan, Murali
- Vicarel, Monica
- Xu, Ruo
- Hyde, Lynn A.
- Del Vecchio, Robert A.
- Cohen-Williams, Mary E.
- Song, Lixin
- Lee, Julie
- Terracina, Giuseppe
- Zhang, Qi
- Nomeir, Amin
- Parker, Eric M.
- Zhang, Lili
- Titel
- Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.844-849
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2013
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (−)-1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer’s disease. Specifically, 4-CF3 and 4-Br substituted arylsulfone analogs, (−)-1b and (−)-1c, are equipotent to compound (−)-1a. On the right hand side chain, linker size and terminal substituents of the pendant sulfone group are also investigated.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2012.11.047Titel-ID: cdi_proquest_miscellaneous_1273494010
- Format
- –
- Schlagworte
- Alzheimer disease, Alzheimer’s disease, Amyloid Precursor Protein Secretases - antagonists & inhibitors, Benzopyrans - chemical synthesis, Benzopyrans - chemistry, Benzopyrans - pharmacology, Cyclization, drugs, Enzyme Activation - drug effects, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, Humans, Inhibitory Concentration 50, Molecular Structure, proteinase inhibitors, proteinases, Pyrans - chemical synthesis, Pyrans - chemistry, Pyrans - pharmacology, Structure activity relationship, structure-activity relationships, Sulfone, Sulfones - chemical synthesis, Sulfones - chemistry, Sulfones - pharmacology, γ-Secretase inhibitor