Matches in SemOpenAlex for { <https://semopenalex.org/work/W2896525391> ?p ?o ?g. }
- W2896525391 endingPage "13666" @default.
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- W2896525391 abstract "We have explored orally effective thyrotropin-releasing hormone (TRH) mimetics, showing oral bioavailability and brain penetration by structure–activity relationship (SAR) study on the basis of in vivo antagonistic activity on reserpine-induced hypothermia in mice. By primary screening of the synthesized TRH mimetics, we found a novel TRH mimetic: l-pyroglutamyl-[3-(thiazol-4-yl)-l-alanyl]-l-prolinamide with a high central nervous system effect compared with TRH as a lead compound. Further SAR optimization studies of this lead compound led to discovery of a novel orally effective TRH mimetic: 1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine trihydrate (rovatirelin hydrate), which was selected as a candidate for clinical trials." @default.
- W2896525391 created "2018-10-26" @default.
- W2896525391 creator A5000256757 @default.
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- W2896525391 creator A5047339634 @default.
- W2896525391 creator A5077612040 @default.
- W2896525391 creator A5084904968 @default.
- W2896525391 date "2018-10-19" @default.
- W2896525391 modified "2023-09-26" @default.
- W2896525391 title "Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1-{<i>N</i>-[(4<i>S</i>,5<i>S</i>)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-<scp>l</scp>-alanyl}-(2<i>R</i>)-2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate)" @default.
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