Author/Authors :
Toshio Nagase، نويسنده , , Toshiaki Mase، نويسنده , , Takehiro Fukami، نويسنده , , Takashi Hayama، نويسنده , , Kagari Fujita، نويسنده , , Kenji Niiyama، نويسنده , , Hirobumi Takahashi، نويسنده , , Uno Kumagai، نويسنده , , Yuko Urakawa، نويسنده , , Yohko Nagasawa، نويسنده , , Masaki Ihara، نويسنده , , Masaru Nishikibe، نويسنده , , Kiyofumi Ishikawa، نويسنده ,
Abstract :
Novel linear tripeptides possessing high endothelin antagonist activity were derived from endothelin antagonistic cyclic pentapeptides represented by BQ-123. The N-terminal urea moiety of the linear tripeptide derivatives was essential to show the strong antagonist activity. An easy method to prepare these peptides by treatment of the corresponding N-phenoxycarbonylated tripeptide esters with primary or secondary amines is described.