Abstract
ABSTRACTIntroduction: alpha 7 subtype nicotinic acetylcholine receptor (α7 nAChR) ligands, that is, ligands that interact with the orthosteric or allosteric binding sites of α7 nAChR, hold great potential for several therapeutic applications. Numerous compounds have been designed targeting α7 nAChR but most of them cannot be used therapeutically for various reasons.Areas covered: The patent application describes a series of germinal substituted aminobenzisoxazole compounds as α7 nAChR ligands. These compounds were claimed as potential therapeutics for treating and/or improving cognitive function. All of the (R)-stereoisomer presented high binding activities for α7 nAChR and several compounds displayed excellent selectivity over 5-HT3R.Expert opinion: The privileged structure-derived modification via bioisosterism and scaffold hopping is an important approach for seeking novel α7 nAChR ligands. The claimed germinal substituted aminobenzisoxazole derivatives with low tPSA values as well as low number of hydrogen bond donors and acceptors are supposed to have sufficient BBB penetration. Although there is a lack of essential biological data and the molecular mechanisms are not clear, these compounds stand for a new type of α7 nAChR ligands and deserve further studies.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
