1192164-09-2Relevant 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.
5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE COMPOUND
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Page/Page column 23, (2011/05/16)
The present invention provides compounds which promote erythropoietin production. Compounds represented by the following general formula (1) or pharmacologically acceptable salts thereof are provided: [wherein, R1 represents a group —X-Q1, X-Q1-Y-Q2 or X-Q1-Y-Q2-Z-Q3, X represents a single bond, —CH2— or the like, Q1 represents a monocyclic or bicyclic heterocyclic group which may have substituent(s), Y represents a single bond, —CH2—, or the like, Q2 represents a monocyclic or bicyclic hydrocarbon ring group which may have substituent(s) or a monocyclic or bicyclic heterocyclic group which may have substituent(s), Z represents a single bond, —CR11R12— or the like, R11 and R12 each independently represents a hydrogen atom, a halogen atom or the like, Q3 represents a phenyl group which may have substituent(s), a C3-C7 cycloalkyl group which may have substituent(s), a C3-C7 cycloalkenyl group which may have substituent(s) or a monocyclic or bicyclic heterocyclic group which may have substituent(s), R2 represents a C1-C3 alkyl group or the like, and R3 represents a hydrogen atom or a methyl group].