PRICE S A, MAMALIS P, McHALE D, GREEN J
Br J Pharmacol Chemother. 1960 Jun;15(2):243-6. doi: 10.1111/j.1476-5381.1960.tb01238.x.
A series of compounds containing an amino-oxy-group has been examined for antibacterial and antifungal activity. The amino-oxy-acids and the alkoxyamines showed little activity, but the hydrazides, notably the amino-oxydodecyl and the amino-oxytetradecyl compounds, had appreciable activity against Staphylococcus aureus. The alkoxydiguanides showed considerable bactericidal activity in vitro against Gram-positive and Gram-negative organisms and some activity against Mycobacterium tuberculosis. The most active compounds were those with a chain containing 10 to 14 carbon atoms, but the activity was considerably reduced in the presence of serum. They were also active against the few fungi tested. The most active compound, decyloxydiguanide, was moderately toxic when administered intraperitoneally to mice and no therapeutic activity could be demonstrated against an intraperitoneal injection of Streptococcus pyogenes administered 15 min. previously.
对一系列含有氨氧基的化合物进行了抗菌和抗真菌活性检测。氨氧基酸和烷氧基胺显示出微弱的活性,但酰肼,特别是氨氧基十二烷基和氨氧基十四烷基化合物,对金黄色葡萄球菌具有明显的活性。烷氧基双胍在体外对革兰氏阳性菌和革兰氏阴性菌显示出相当大的杀菌活性,对结核分枝杆菌也有一定活性。活性最高的化合物是那些碳链含有10至14个碳原子的化合物,但在血清存在下活性会大幅降低。它们对所测试的少数真菌也有活性。活性最高的化合物癸氧基双胍,腹腔注射给小鼠时具有中等毒性,对15分钟前腹腔注射的化脓性链球菌没有显示出治疗活性。