New Advances in Chemical Research in 2021. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. Computed Properties of C8H5BrS, In an article, mentioned the application of 4923-87-9, Name is 5-Bromobenzothiophene, molecular formula is C8H5BrS
Recent studies have suggested that the alpha7 nicotinic acetylcholine receptors play important roles in learning and memory. Herein, we describe our research of the structure-activity relationships (SAR) in a series of (5)-spiro[1-azabicyclo[2.2.2]octane-3,5?-oxazolidin]-2?-ones bearing various bicyclic moieties to discover novel ?7 receptor agonists. Through a number of SAR studies on the series, we have found out that inhibition of CYP 2D6 isozyme, which was a primary obstacle for the previously identified compound, was avoidable by the introduction of bicyclic moieties. Chemical optimization of the series led to the identification of a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist 23. This compound not only possessed high binding affinity (Ki = 3 nmol/L) toward the alpha7 receptor but also showed agonistic activity even at a concentration of 0.1 mumol/L. In addition, compound 23 improved cognition in several rat models, which might suggest the potential of the alpha7 receptor partial agonist for the treatment of neurological disorders including cognitive dysfunction.
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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem