UROTENSIN-II AGONISTS AND ANTAGONISTS Russian patent published in 2005 - IPC

FIELD: organic chemistry, polypeptides.

SUBSTANCE: invention relates to new antagonists of urotensin-II. Invention represents group of cyclic polypeptides of the general formula: (R¹)_a-AA¹-cyclo-[AA²-AA³-AA⁴-AA⁵-AA⁶-Cys]-AA⁷-R² wherein AA¹ means L-isomer of aromatic amino acid; AA² means L- or D-isomer of Cys; AA³ means L-isomer of aromatic amino acid; AA⁴ means L- or D-isomer of Trp; AA⁵ means L- or D-isomer of Lys, N-Me-Lys or Orn; AA⁶ means L- or D-isomer of Val, Thr, Leu, Ile, Tle, Nle or aromatic amino acid; AA⁷ means L- or D-isomer of Val, Thr, Leu, Ile, Tle, Abu, Nle or aromatic amino acid; R¹ means hydrogen atom (H), lower alkyl, lower alkanoyl or lower acyl; a = 1 or 2; R² means hydroxyl; group (OH), OR³, N(R³)₂ or NHR³ wherein R³ means H, lower alkyl or arylalkyl. These cyclic polypeptides are used as antagonists of urotensin-II.

EFFECT: valuable biological properties of compounds.

24 cl, 1 tbl, 2 ex