GLYCINE DERIVATIVES OR THEIR PHYSIOLOGICALLY ACCEPTABLE SALTS SHOWING CAPABILITY TO INHIBIT FIBRINOGEN BINDING IN FIBRINOGEN PLATELET RECEPTOR

摘要

FIELD: organic chemistry. SUBSTANCE: derivatives of glycine of the general formula (I) R-CONH-CH₂CONHCH(R)CH₂COOH where R - a group of formula -CH(NHR^a)-(CH₂)_1-6NH-R^b (R-1), (T)_m-C₆H₄CH₂NH₂ (R-2), (T)_m-C₆H₄(NH)_nC(NH)-L (R-3) or (R-4) where R^a - hydrogen, -COOC₁-C₄-alkyl, Z, -COC₅H₄N₃, -SO₂-naphthyl or -COCH₂H(Y)CH₂CH₂NH-Y where Y - hydrogen, Boc or Z; R^b - a group of the formula -C(NH)(CH₂)_0-3CH₃ or , or if R^a a group of the formula -COC₆H₄N₃, -SO₂ -naphthyl or -COCH₂N(Y)CH₂CH₂NHY then R^b - amidino-group where n = 1 or O, L - amino-group, or if n = 1 then L is also -(CH₂)_0-3-CH₃; T - a group of the formula -CH₂-(O)_n, n = 1 or -CH(R^d)-CH₂ or -CH₂CO-; one of carbonyl-group in T-group can be in the form of ketal; R^d - hydrogen or NHR^a or R=H, or COR⁰, R⁰- -NH0C_1-4 -alkyl, -NH(CH₂)_1-4-C₀H₄Hal, -NHC₀H₄COOH, or radical linked over amino-group of -aminocarboxylic acid, or their physiologically acceptable salt. Reagent 1: compound of indicated above formula with protected amino-groups: Phe, Ala - t-butylhydroxycarbonyl, Asp, Val - ot-butyl, Arg-benzylhydroxycarbonyl, Ala - benzyl. Reagent 2: clearing one. Synthesized compounds show low toxicity and show high capability to inhibit fibrinogen binding. Synthesized compounds are used in biochemistry. EFFECT: enhanced effectiveness of compounds indicated above. 1 tbl