114432-13-2Relevant articles and documents
COMPOUNDS FOR INHIBITING BETA-AMYLOID PRODUCTION
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, (2008/06/13)
Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of the compounds. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of the compounds.
A Novel Class of Calcium-Entry Blockers: The 1-sulfonyl>indolizines
Gubin, Jean,Lucchetti, Jean,Mahaux, Jean,Nisato, Dino,Rosseels, Gilbert,et al.
, p. 981 - 988 (2007/10/02)
The synthesis and initial biological evaluation of a series of 1-sulfonylindolizines is described.These compounds have been shown to be representatives of a novel class of potent, slow-channel calcium antagonists.All compounds were found to be at least as active as the reference calcium antagonists verapamil and cis-(+)-diltiazem.Structure-activity relationship studies have shown that all compounds possessing an aralkyl group in the amine moiety and an isopropyl or cyclopropyl group at the 2 position of the indolizine are among the most potent calcium antagonists know n outside the 1,4-dihydropyridine series.The IC50 value for the inhibition of nitrendipine binding vary between o.19 and 4.5 nM whereas the IC50 value for nifedipine is 2.5 nM.One of the compounds in this group (9ab) has now been selected for clinical development.
