Matches in SemOpenAlex for { <https://semopenalex.org/work/W2772090296> ?p ?o ?g. }
- W2772090296 endingPage "984" @default.
- W2772090296 startingPage "979" @default.
- W2772090296 abstract "6,7-Dihydro-5H-2,1-benzisoxazol-4-one analogs are potent inhibitors of aldosterone synthase (CYP11B2) with selectivity over the highly homologous enzyme cortisol synthase (CYP11B1). These compounds are unique among inhibitors of CYP11B2 in their lack of a strong-heme binding group such as a pyridine or imidazole. Poor metabolic stability in hepatocyte incubations was found to proceed via a reduction of the isoxazole ring. While the enzyme responsible for the reductive metabolism remains unknown, the rate of metabolism could be attenuated by the addition of polar functionality. The in vitro CYP11B2 potency and selectivity were confirmed in vivo in a cynomolgus monkey model by the inhibition of ACTH stimulated aldosterone production without impacting plasma cortisol concentrations." @default.
- W2772090296 created "2017-12-22" @default.
- W2772090296 creator A5001601904 @default.
- W2772090296 creator A5004066610 @default.
- W2772090296 creator A5006230180 @default.
- W2772090296 creator A5006657942 @default.
- W2772090296 creator A5010123902 @default.
- W2772090296 creator A5014559806 @default.
- W2772090296 creator A5015449000 @default.
- W2772090296 creator A5021750788 @default.
- W2772090296 creator A5022983409 @default.
- W2772090296 creator A5034092266 @default.
- W2772090296 creator A5044214752 @default.
- W2772090296 creator A5045924594 @default.
- W2772090296 creator A5047630189 @default.
- W2772090296 creator A5047706126 @default.
- W2772090296 creator A5052389581 @default.
- W2772090296 creator A5058765353 @default.
- W2772090296 creator A5061818587 @default.
- W2772090296 creator A5064095073 @default.
- W2772090296 creator A5064383790 @default.
- W2772090296 creator A5074720637 @default.
- W2772090296 creator A5080160667 @default.
- W2772090296 creator A5084055397 @default.
- W2772090296 creator A5086113874 @default.
- W2772090296 creator A5089061216 @default.
- W2772090296 creator A5089645848 @default.
- W2772090296 date "2018-03-01" @default.
- W2772090296 modified "2023-09-26" @default.
- W2772090296 title "Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity" @default.
- W2772090296 cites W1126044527 @default.
- W2772090296 cites W1882449366 @default.
- W2772090296 cites W1991306589 @default.
- W2772090296 cites W2003715315 @default.
- W2772090296 cites W2010799694 @default.
- W2772090296 cites W2028105139 @default.
- W2772090296 cites W2044773944 @default.
- W2772090296 cites W2050561069 @default.
- W2772090296 cites W2055851367 @default.
- W2772090296 cites W2056976690 @default.
- W2772090296 cites W2067956701 @default.
- W2772090296 cites W2082983286 @default.
- W2772090296 cites W2104114105 @default.
- W2772090296 cites W2116841159 @default.
- W2772090296 cites W2126846194 @default.
- W2772090296 cites W2130479394 @default.
- W2772090296 cites W2132715232 @default.
- W2772090296 cites W2138101271 @default.
- W2772090296 cites W2146496405 @default.
- W2772090296 cites W2148589377 @default.
- W2772090296 cites W2416601434 @default.
- W2772090296 cites W2487079562 @default.
- W2772090296 doi "https://doi.org/10.1016/j.bmcl.2017.12.015" @default.
- W2772090296 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29254646" @default.
- W2772090296 hasPublicationYear "2018" @default.
- W2772090296 type Work @default.
- W2772090296 sameAs 2772090296 @default.
- W2772090296 citedByCount "7" @default.
- W2772090296 countsByYear W27720902962018 @default.
- W2772090296 countsByYear W27720902962019 @default.
- W2772090296 countsByYear W27720902962020 @default.
- W2772090296 countsByYear W27720902962021 @default.
- W2772090296 countsByYear W27720902962023 @default.
- W2772090296 crossrefType "journal-article" @default.
- W2772090296 hasAuthorship W2772090296A5001601904 @default.
- W2772090296 hasAuthorship W2772090296A5004066610 @default.
- W2772090296 hasAuthorship W2772090296A5006230180 @default.
- W2772090296 hasAuthorship W2772090296A5006657942 @default.
- W2772090296 hasAuthorship W2772090296A5010123902 @default.
- W2772090296 hasAuthorship W2772090296A5014559806 @default.
- W2772090296 hasAuthorship W2772090296A5015449000 @default.
- W2772090296 hasAuthorship W2772090296A5021750788 @default.
- W2772090296 hasAuthorship W2772090296A5022983409 @default.
- W2772090296 hasAuthorship W2772090296A5034092266 @default.
- W2772090296 hasAuthorship W2772090296A5044214752 @default.
- W2772090296 hasAuthorship W2772090296A5045924594 @default.
- W2772090296 hasAuthorship W2772090296A5047630189 @default.
- W2772090296 hasAuthorship W2772090296A5047706126 @default.
- W2772090296 hasAuthorship W2772090296A5052389581 @default.
- W2772090296 hasAuthorship W2772090296A5058765353 @default.
- W2772090296 hasAuthorship W2772090296A5061818587 @default.
- W2772090296 hasAuthorship W2772090296A5064095073 @default.
- W2772090296 hasAuthorship W2772090296A5064383790 @default.
- W2772090296 hasAuthorship W2772090296A5074720637 @default.
- W2772090296 hasAuthorship W2772090296A5080160667 @default.
- W2772090296 hasAuthorship W2772090296A5084055397 @default.
- W2772090296 hasAuthorship W2772090296A5086113874 @default.
- W2772090296 hasAuthorship W2772090296A5089061216 @default.
- W2772090296 hasAuthorship W2772090296A5089645848 @default.
- W2772090296 hasConcept C112243037 @default.
- W2772090296 hasConcept C134018914 @default.
- W2772090296 hasConcept C150903083 @default.
- W2772090296 hasConcept C155392382 @default.
- W2772090296 hasConcept C181199279 @default.
- W2772090296 hasConcept C185592680 @default.
- W2772090296 hasConcept C198710026 @default.
- W2772090296 hasConcept C202751555 @default.
- W2772090296 hasConcept C207001950 @default.