Department of Materials and Life Science, Faculty of Science and Technology, Seikei University, 3-3-1, Kichijoji-kitamachi, Musashino, Tokyo 180-8633, Japan.
Bioorg Chem. 2012 Apr-Jun;41-42:1-5. doi: 10.1016/j.bioorg.2011.12.002. Epub 2011 Dec 29.
We synthesized 12 derivatives of 2,3-bis(bromomethyl)quinoxaline with substituents at the 6- and/or 7-positions, and evaluated their activities against bacteria and fungi. Of the 12 compounds, nine (1a-h, 1j, and 1k) showed antibacterial activity. The derivative 1g, which bears a trifluoromethyl group at the 6-position, showed the highest activity against Gram-positive bacteria, while 1c, which has a fluoro-group at the 6-position, showed the widest antifungal activity spectrum. However, only the derivative with an ethyl ester substitution, 1k showed activity against Gram-negative bacteria.
我们合成了 12 种 2,3-双（溴甲基）喹喔啉衍生物，这些衍生物在 6-和/或 7-位带有取代基，并评估了它们对细菌和真菌的活性。在这 12 种化合物中，有 9 种（1a-h、1j 和 1k）具有抗菌活性。在 6 位带有三氟甲基取代基的衍生物 1g 对革兰氏阳性菌表现出最高的活性，而在 6 位带有氟基团的 1c 则表现出最广泛的抗真菌活性谱。然而，只有带有乙酯取代基的衍生物 1k 对革兰氏阴性菌具有活性。
