| 摘要 |
Guanidine derivatives of the formula:-
Het<1>-(CH2)m-Y<1>-(CH2)n-NR<1>-A-NR<2>-(CH2)g- Y<2>-(CH2)p- Het<2> (I)
in which Y<1> and Y<2> are O, S, direct bonds, CH2 or SO; m and p are 0 to 4, n and g are 1 to 4, provided that when Y<1> or Y<2> is 0, S or SO, m or p is 1 to 4 and provided that when Y<1> or Y<2> is 0 or SO, n or g is 2 to 4; one of R<1> and R<2> is hydrogen and the other is hydrogen or C(1-6)alkyl; A is e.g. 3,4-dioxocyclobuten-1, 2-diyl or C = Z in which Z is S, O, NCN, NNO2, CHNO2, NCONH2, C(CN)2 or NH;
Het<1> is cayzol-4-yl, thiazol-4-yl or imidazol-4-yl substituted in the 2-position by:-
<CHEM>
or Het<1> is 1,2,4-thiadiazol-3-yl or 1,2,4-oxadiazol-3-yl substituted in the 5-position by radical III in which R<5> is hydrogen, C(1-10)alkyl, C(1-6)alkanoyl or C(7-11)aroyl; Het<2> is e.g. same as Het<1> or an optionally substituted unfused N-containing 5- or 6-membered monocyclic heterocyclic ring; provided that when R<1> and R<2> are hydrogen and A is C = NH, Y<1> and/or Y<2> is S, and that when R<1> and R<2> are hydrogen; A is C = NH and Het<2> is imidazole, the number of atoms in the chain:-
(CH2)g-Y<2>-(CH2)p
is at least 4;
and salts thereof. The process of manufacture of said compounds is described; e.g. 2-guanidino-4[(2-aminoethyl)thiomethyl]thiazole gives by reaction with carbon disulphide 1,3-bis[2- (2-guanidino-thiazol-4- ylmethylthio)ethyl]-thiourea. |
