Synthetic routes are described to a series of 2-, 6- and 8- phenylpurines , each with an appropriate S-or NH-linked side chain elsewhere in the molecule; to 2- and 4-phenylpteridines, each with a similar side chain and some with two additional C-methyl groups, to 2- and 4-phenylquinazolines, each equipped with an analogous side chain; and to two pyridinyl analogues of the above. Three of the above components are shown to have considerable activity as amplifiers of phleomycin -G in an in vitro bacterial system.
本研究描述了一系列 2-、6-和 8-苯基嘌呤的合成路线,每种嘌呤在分子的其他部位都有适当的 S 或 NH 链接侧链;2-和 4-苯基蝶啶,每种蝶啶都有类似的侧链,有些蝶啶还带有两个额外的 C-甲基;2-和 4-苯基喹唑啉,每种喹唑啉都带有类似的侧链;以及上述喹唑啉的两种吡啶类似物。在体外细菌系统中,上述成分中的三种被证明具有相当高的活性,可作为 phleomycin -G 的扩增剂。