202002-66-2Relevant articles and documents
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.
Corresponding amine nitrile and method of manufacturing thereof
-
Paragraph 0153; 0154; 0155; 0166; 0167, (2018/05/07)
The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
5-HT7 RECEPTOR ANTAGONISTS
-
Page/Page column 18, (2009/05/28)
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is C(H)= or -N= and R1-7 are as defined herein.