Castelli M, Genedani S, Bertolini A
Chemotherapy. 1979;25(2):91-5. doi: 10.1159/000237828.
2-Amino-4-methyl-6-(2-ethinyl-5-nitrofuryl)-pyrimidine (nifurpyrimidine) is a new furan derivative. Its spectrum of activity is wide and includes both gram-positive and gram-negative microorganisms and fungi; moreover, it inhibits the growth of multiple-drug resistant salmonellae. The minimal inhibitory concentrations ranged from 0.25 to 10 microgram/ml. Resistance was developed in vitro in a step-wise manner and was partially reversed after 7-10 passages in drug-free media. The pharmacological study of the drug was carried out in rats and mice and gave the following results: (1) no acute toxicity was demonstrable following oral administration; (2) no intestinal absorption occurred and virtually the whole dose of nifurpyrimidine administered by oral route was recovered in the intestinal content; (3) the presence of urine, plasma or feces did not modify the antibacterial activity of the compound.
2-氨基-4-甲基-6-(2-乙炔基-5-硝基呋喃基)-嘧啶(硝呋嘧啶)是一种新型呋喃衍生物。其活性谱广泛,包括革兰氏阳性菌、革兰氏阴性菌和真菌;此外,它还能抑制多重耐药沙门氏菌的生长。最小抑菌浓度范围为0.25至10微克/毫升。在体外逐步产生耐药性,在无药培养基中传代7至10次后耐药性部分逆转。在大鼠和小鼠身上进行了该药物的药理学研究,结果如下:(1)口服给药后未显示出急性毒性;(2)未发生肠道吸收,口服给予的硝呋嘧啶几乎全部剂量在肠道内容物中回收;(3)尿液、血浆或粪便的存在不改变该化合物的抗菌活性。