2009
DOI: 10.1016/j.bmcl.2009.10.060
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N-Bridged bicyclic sulfonamides as inhibitors of γ-secretase

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Cited by 10 publications
(5 citation statements)
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“…Thus, the quinoline series 1 ostensibly offered the lowest hurdle to prepare metabolically stable inhibitors. This series had a single aliphatic carbon (the site of oxidation), whereas both the piperidine 2 and bicyclic 3 series bore multiple aliphatic carbons as potential sites for oxidation (see refs and for early development of the series).…”
Section: Results Discussion and Chemistrymentioning
confidence: 99%
“…Thus, the quinoline series 1 ostensibly offered the lowest hurdle to prepare metabolically stable inhibitors. This series had a single aliphatic carbon (the site of oxidation), whereas both the piperidine 2 and bicyclic 3 series bore multiple aliphatic carbons as potential sites for oxidation (see refs and for early development of the series).…”
Section: Results Discussion and Chemistrymentioning
confidence: 99%
“…In summary, the in vivo selectivity of ELN475516 from a mouse seven-day safety model corroborates the improved selectivity estimated for this compound in the cellular SNC assay, confirming APP selective inhibition of gamma-secretase in vivo by this novel pyrazolylazabicyclo(3.3.1)nonane sulfonamide. ELN475156 represents a validated foundation for further lead optimization to discover APP selective second generation GSIs with improved safety and drug like properties suitable for chronic AD therapy [60,98,103,104]. …”
Section: Discussionmentioning
confidence: 99%
“…Sulfonamides also have substantial value in the treatment of more complex diseases. After the belief that sulfonamide derivatives could have enzyme inhibitor residences in a broad variety of biological pathways, they have been applied as carbonic anhydrase inhibitors (CAI) in diverse applications as well as anti-hyperthyroidism, antitumor and anticancer agents [150][151][152][153][154][155][156][157].…”
Section: Fig 33; G-sphingosine Kinase Inhibitorsmentioning
confidence: 99%
“…Inside the beyond decade, there have been substantial new tendencies in drug discovery closer to the treatment of dementia and Alzheimer's disease using sulfonamide derivatives in multi-target procedures. Following the work of [150] on Nbridged bicyclic sulfonamide-based inhibitors of γsecretase as new anti-AD drug candidates, the attention was divided between γ-secretase inhibition to prevent amyloid β accumulation and inhibition of two cholinesterase enzymes of the cholinergic system that is responsible for neurotransmission and is related to memory and other cognitive activities.…”
Section: I-alzheimer's Diseasementioning
confidence: 99%