Matches in SemOpenAlex for { <https://semopenalex.org/work/W2023511051> ?p ?o ?g. }
- W2023511051 endingPage "1870" @default.
- W2023511051 startingPage "1865" @default.
- W2023511051 abstract "A novel class of human β3-adrenergic receptor agonists was designed in effort to improve selectivity and metabolic stability versus previous disclosed β3-AR agonists. As observed, many of the β3-AR agonists seem to need the acyclic ethanolamine core for agonist activity. We have synthesized derivatives that constrained this moiety by introduction of a pyrrolidine. This unique modification maintains human β3 functional potency with improved selectivity versus ancillary targets and also eliminates the possibility of the same oxidative metabolites formed from cleavage of the N–C bond of the ethanolamine. Compound 39 exhibited excellent functional β3 agonist potency across species with good pharmacokinetic properties in rat, dog, and rhesus monkeys. Early de-risking of this novel pyrrolidine core (44) via full AMES study supports further research into various new β3-AR agonists containing the pyrrolidine moiety." @default.
- W2023511051 created "2016-06-24" @default.
- W2023511051 creator A5003058999 @default.
- W2023511051 creator A5006012041 @default.
- W2023511051 creator A5011500193 @default.
- W2023511051 creator A5024370387 @default.
- W2023511051 creator A5025998077 @default.
- W2023511051 creator A5036158401 @default.
- W2023511051 creator A5038451924 @default.
- W2023511051 creator A5040673831 @default.
- W2023511051 creator A5042308407 @default.
- W2023511051 creator A5043413150 @default.
- W2023511051 creator A5044677569 @default.
- W2023511051 creator A5047332534 @default.
- W2023511051 creator A5050475544 @default.
- W2023511051 creator A5053478547 @default.
- W2023511051 creator A5056532797 @default.
- W2023511051 creator A5056881284 @default.
- W2023511051 creator A5056987410 @default.
- W2023511051 creator A5062855575 @default.
- W2023511051 creator A5063656478 @default.
- W2023511051 creator A5065280044 @default.
- W2023511051 creator A5067596354 @default.
- W2023511051 creator A5071587293 @default.
- W2023511051 creator A5089399451 @default.
- W2023511051 date "2011-03-01" @default.
- W2023511051 modified "2023-10-04" @default.
- W2023511051 title "Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists" @default.
- W2023511051 cites W1941976899 @default.
- W2023511051 cites W1966574695 @default.
- W2023511051 cites W1968220874 @default.
- W2023511051 cites W1973849801 @default.
- W2023511051 cites W1973879072 @default.
- W2023511051 cites W1996768696 @default.
- W2023511051 cites W2002292710 @default.
- W2023511051 cites W2002896923 @default.
- W2023511051 cites W2004120839 @default.
- W2023511051 cites W2004722122 @default.
- W2023511051 cites W2007886796 @default.
- W2023511051 cites W2015912619 @default.
- W2023511051 cites W2019100110 @default.
- W2023511051 cites W2021289165 @default.
- W2023511051 cites W2045354334 @default.
- W2023511051 cites W2065027603 @default.
- W2023511051 cites W2093273801 @default.
- W2023511051 cites W2094871139 @default.
- W2023511051 cites W2121162804 @default.
- W2023511051 cites W2121960800 @default.
- W2023511051 cites W2123251006 @default.
- W2023511051 cites W2126137471 @default.
- W2023511051 cites W2129787793 @default.
- W2023511051 cites W2139904173 @default.
- W2023511051 cites W2159960984 @default.
- W2023511051 cites W2161566985 @default.
- W2023511051 cites W2162150396 @default.
- W2023511051 cites W2165752411 @default.
- W2023511051 cites W2317312447 @default.
- W2023511051 cites W2464682502 @default.
- W2023511051 doi "https://doi.org/10.1016/j.bmcl.2010.12.087" @default.
- W2023511051 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21353541" @default.
- W2023511051 hasPublicationYear "2011" @default.
- W2023511051 type Work @default.
- W2023511051 sameAs 2023511051 @default.
- W2023511051 citedByCount "11" @default.
- W2023511051 countsByYear W20235110512013 @default.
- W2023511051 countsByYear W20235110512014 @default.
- W2023511051 countsByYear W20235110512016 @default.
- W2023511051 countsByYear W20235110512017 @default.
- W2023511051 countsByYear W20235110512019 @default.
- W2023511051 countsByYear W20235110512022 @default.
- W2023511051 countsByYear W20235110512023 @default.
- W2023511051 crossrefType "journal-article" @default.
- W2023511051 hasAuthorship W2023511051A5003058999 @default.
- W2023511051 hasAuthorship W2023511051A5006012041 @default.
- W2023511051 hasAuthorship W2023511051A5011500193 @default.
- W2023511051 hasAuthorship W2023511051A5024370387 @default.
- W2023511051 hasAuthorship W2023511051A5025998077 @default.
- W2023511051 hasAuthorship W2023511051A5036158401 @default.
- W2023511051 hasAuthorship W2023511051A5038451924 @default.
- W2023511051 hasAuthorship W2023511051A5040673831 @default.
- W2023511051 hasAuthorship W2023511051A5042308407 @default.
- W2023511051 hasAuthorship W2023511051A5043413150 @default.
- W2023511051 hasAuthorship W2023511051A5044677569 @default.
- W2023511051 hasAuthorship W2023511051A5047332534 @default.
- W2023511051 hasAuthorship W2023511051A5050475544 @default.
- W2023511051 hasAuthorship W2023511051A5053478547 @default.
- W2023511051 hasAuthorship W2023511051A5056532797 @default.
- W2023511051 hasAuthorship W2023511051A5056881284 @default.
- W2023511051 hasAuthorship W2023511051A5056987410 @default.
- W2023511051 hasAuthorship W2023511051A5062855575 @default.
- W2023511051 hasAuthorship W2023511051A5063656478 @default.
- W2023511051 hasAuthorship W2023511051A5065280044 @default.
- W2023511051 hasAuthorship W2023511051A5067596354 @default.
- W2023511051 hasAuthorship W2023511051A5071587293 @default.
- W2023511051 hasAuthorship W2023511051A5089399451 @default.
- W2023511051 hasConcept C170493617 @default.
- W2023511051 hasConcept C185592680 @default.
- W2023511051 hasConcept C202751555 @default.