1159982-27-0Relevant academic research and scientific papers
Structure-activity relationship study of tryptophan-based butyrylcholinesterase inhibitors
Brazzolotto, Xavier,Gobec, Stanislav,Gro?elj, Uro?,Knez, Damijan,Malikowska-Racia, Natalia,Meden, An?e,Nachon, Florian,Sa?at, Kinga,Svete, Jurij
, (2020/09/15)
A series of tryptophan-based selective nanomolar butyrylcholinesterase (BChE) inhibitors was designed and synthesized. Compounds were optimized in terms of potency, selectivity, and synthetic accessibility. The crystal structure of the inhibitor 18 in complex with BChE revealed the molecular basis for its low nanomolar inhibition (IC50 = 2.8 nM). The favourable in vitro results enabled a first-in-animal in vivo efficacy and safety trial, which demonstrated a positive impact on fear-motivated and spatial long-term memory retrieval without any concomitant adverse motor effects. Altogether, this research culminated in a handful of new lead compounds with promising potential for symptomatic treatment of patients with Alzheimer's disease.
FUSED BICYCLIC COMPOUND FOR INHIBITING ACTIVITY OF TYROSINE KINASE
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Paragraph 0137; 0138, (2019/06/12)
A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation and use thereof are disclosed. In particular, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydr
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00306, (2017/09/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
