| 摘要 |
Amidine derivs. of formula R3-NH-C(=NR1)-R-COR2 (I) and their salts are new. R = -Q-B-Q1-(CH2)n-, -Q-CH2-O-Phe-(CH2)p-, -Q-CH2-O-Phe-CH2-CH(NHR4)-, -Phe-NHCOCH2CH2CONHCHR5CH2-, -Phe-Q2(CH2)k-Q3-(CH2)l-, -Phe-CO-AA-Q4-OCH2-, -Phe-Phe-OCH2-Q5-CH2-, -Phe-NR6CO-Q6-(CH2)m-, -Phe-CONR8-CH2COQ7O(CH2)n or -Q4-(CH2)p-O-Phe-CH2-CH(NHR4)-; Q = a gp. of formula (q); Q1 = a gp. of formula (a) or (b); Q2, Q3 = a gp. of formula (c); Q4 = a gp. of formula (c; D = N; E = CH); Q5 = a gp. of formula (d); Q6 = a gp. of formula (e); Q7 = a gp. of formula (f); B = CH2, CO or CS; R10 = OH or H; m = 0-4; U = CH2 or CO; R9 = H, CO2H or CO2A; n = 0-3; p = 1-4; R4 = H, SO2A, SO2Ar, COA, COAr or COHet; R5 = H, A, 2-5C alkinyl, 2-5C alkenyl or Ar; D, E = CH or N; k, l = 0-4; AA = amino-acid residue from Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr or Val; R6 = H or A; R7 = OH, OA, OAr, OHet, NHOH or NA2; R8 = H or A; p = 1-4; q = 2-6; R1 = H, A, COAr, COA, OH, OA or COOA; R2 = OH, OA, OAr, OHet, NHOH, NH2, NHA or NA2; R3 = COA, COAr, COHet, COOHet, COOAr, COOA, SO2Ar or SO2A; A = 1-6C alkyl; Ar = 6-10C aryl, diphenylmethyl or benzyl (all opt. substd. by A, halo, OA, -O-CH2-O-, COOA, COOH, CF3, OH, NO2, CN, NH2, OCOA, NHA or NA2); Het = mono- or bi-cyclic, opt. unsatd. or aromatic heterocycle with 1-4 N, O or S (opt. substd. by F, Cl, Br, CF3, A, OH, OA, CN or NO2): provided that when D, E in Q2 = N then k is not 0; and when D, E = in Q3 and E in Q2 = N, and k = 0; then l is not l. |
