91817-61-7Relevant academic research and scientific papers
Tryptophan-derived butyrylcholinesterase inhibitors as promising leads against Alzheimer's disease
Meden, An?e,Knez, Damijan,Juki?, Marko,Brazzolotto, Xavier,Gr?i?, Marija,Pi?lar, Anja,Zahirovi?, Abida,Kos, Janko,Nachon, Florian,Svete, Jurij,Gobec, Stanislav,Gro?elj, Uro?
supporting information, p. 3765 - 3768 (2019/04/01)
We have identified tryptophan-based selective nanomolar butyrylcholinesterase (BChE) inhibitors. They are defined according to their chemical modularity, novel binding mode revealed by five solved crystal structures with human BChE, low cytotoxicity, and predicted permeability of the blood-brain barrier. Altogether, these factors indicate their potential as unique lead compounds for symptomatic therapy against Alzheimer's disease.
5-HT3 receptor agonist, novel thiazole derivative and intermediate thereof
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, (2008/06/13)
A 5-HT3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): STR1 wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms; one of L1 or L2 represents a single bond and the other is non-existent or represents an alkylene or alkenylene group; R represents: STR2
Model Compounds for the Study of Spectroscopic Properties of Visual Pigments and Bacteriorhodopsin
Baasov, Timor,Sheves, Mordechai
, p. 7524 - 7533 (2007/10/02)
A series of modified retinals bearing nonconjugated positive charges along the polyene were synthesized.It was found that nonconjugated charges shifted the absorption maxima of retinal chromophore as well as protonated retinal Schiff bases.The magnitude of shift observed in bacteriorhodopsin (bR), 5170 cm-1, could be found in our models by the additivity of two factors: (1) interaction through space with a positive charge located in the vicinity of the ring operating in nonprotic solvents, provided that the interaction between the charge and its counteranion is weakened by a homoconjugation effect; (2) weakening the interaction of the Schiff base positively charged nitrogen with its counteranion.A shift of ca. 5000 cm-1 can also be achieved by interaction through space with two nonconjugated positive charges.The absorption maximum of protonated retinal Schiff base is influenced significantly by an interaction with a nonconjugated charge located in the vicinity of the ring moiety or carbon 9.The influence of a charge located in the vicinity of carbon 12 and carbon 14 is minor.Nonconjugated positive charges have a remarkable effect on C=C stretching frequencies as well.It is suggested that the different C=C stretching frequencies found in bR, visual pigments, as well as their photochemically induced intermediates, may originate from interaction with external charges, the C=N+ stretching frequency does no exhibit similar sensitivity to external nonconjugated charges, and it is practically unaffected by them.
