Kobayashi, Naotake; Sato, Norihito; Fujimura, Yuko; Kihara, Tsuyoshi; Sugita, Katsuji; Takahashi, Kouji; Koike, Katsumi; Sugawara, Tamio; Tada, Yukio; Nakai, Hiroshi; Yoshikawa, Takayoshi published the artcile< Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1-{N-[(4S,5S)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-L-alanyl}-(2R)-2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate)>, Computed Properties of 1003-32-3, the main research area is TRH mimetics rovatirelin hydrate synthesis brain disease crystal structure.
We have explored orally effective TSH-releasing hormone (TRH) mimetics showing oral bioavailability and brain penetration by 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 high central nervous system (CNS) effect compared to 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 clin. trials.
ACS Omega published new progress about Bioavailability. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Computed Properties of 1003-32-3.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica