THIS compound (I) was prepared for the following reason: pyridine-3-sulphonic acid and its amide were found to inhibit bacterial growth, apparently by interference with nicotinic acid metabolism1. Sulphanilamide appears to act as a therapeutic agent by interfering with the utilization of p-aminobenzoic acid by the invading organisms2, but the 2-aminopyridine derivative(M. & B. 693) is in many cases more effective. Following a rule of thumb method common in chemotherapeutic research, the M. & B. 693 analogue of pyridine-3-sulphonic acid, (I), was prepared and its inhibitory powers compared with those of the parent acid and amide by in vitro tests analogous to those previously described1,2. The compound was found less active than the simple acid and amide.
制备这种化合物(I)的原因如下:
吡啶-3-
磺酸及其酰胺被发现可以抑制细菌生长,这显然是通过干扰
烟酸代谢实现的1。磺
胺类药物似乎是通过干扰入侵
生物对
对氨基苯甲酸的利用来发挥治疗作用的2,但2-
氨基
吡啶衍生物(M. & B. 693)在许多情况下更有效。根据
化学治疗研究中常用的经验法则,制备了
吡啶-3-
磺酸的M. & B. 693类似物(I),并通过与之前描述的类似的体外试验,将其抑制能力与母体酸和酰胺进行了比较1,2。发现该化合物不如简单的酸和酰胺活性高。