Grivas S, Jägerstad M
Mutat Res. 1984 Jul;137(1):29-32. doi: 10.1016/0165-1218(84)90108-3.
3-Methyl- and 3,4-dimethyl-3H-imidazo[4,5-f]quinoline, 3,8-dimethyl-3H-imidazo[4,5-f]quinoxaline, N6-methyl- and N6,7-dimethylquinoline-5,6-diamine, as well as N6,3-dimethylquinoxaline-5,6-diamine, have been synthesized. Only the first-mentioned compound was active in Ames test; the response was equal for Salmonella typhimurium TA98 and TA100, regardless of enzymatic activation (S9). However, its mutagenicity to TA98 + S9 was 300-1300 times smaller than the values reported for the related compounds, 3-methyl- and 3,4-dimethyl-3H-imidazo[4,5-f]quinolin-2-amine ('IQ' and 'MeIQ'), and for 3,8-dimethyl-3H-imidazo[4,5-f]quinoxalin-2-amine ('MeIQx'). Hence, the presence of the imidazole ring and the 2-amino group in the molecule seems to be important for the high mutagenicity of the latter compounds.
已合成出3-甲基-和3,4-二甲基-3H-咪唑并[4,5-f]喹啉、3,8-二甲基-3H-咪唑并[4,5-f]喹喔啉、N6-甲基-和N6,7-二甲基喹啉-5,6-二胺以及N6,3-二甲基喹喔啉-5,6-二胺。只有上述第一种化合物在艾姆斯试验中有活性；无论有无酶激活（S9），鼠伤寒沙门氏菌TA98和TA100的反应相同。然而，其对TA98 + S9的致突变性比相关化合物3-甲基-和3,4-二甲基-3H-咪唑并[4,5-f]喹啉-2-胺（“IQ”和“MeIQ”）以及3,8-二甲基-3H-咪唑并[4,5-f]喹喔啉-2-胺（“MeIQx”）所报道的值小300 - 1300倍。因此，分子中咪唑环和2-氨基的存在似乎对后几种化合物的高致突变性很重要。
