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新型硝基呋喃2-氨基-4-甲基-6-(2-乙炔基-5-硝基呋喃基)嘧啶(硝呋嘧啶)在小鼠和大鼠身上的微生物学和药理学评价

Microbiological and pharmacological evaluation, in mice and rats, of a new nitrofuran: 2-amino-4-methyl-6-(2-ethinyl-5-nitrofuryl)-pyrimidine (nifurpyrimidine).

作者信息

Castelli M, Genedani S, Bertolini A

出版信息

Chemotherapy. 1979;25(2):91-5. doi: 10.1159/000237828.

DOI:10.1159/000237828
PMID:446189
Abstract

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.

摘要

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。

相似文献

1
Microbiological and pharmacological evaluation, in mice and rats, of a new nitrofuran: 2-amino-4-methyl-6-(2-ethinyl-5-nitrofuryl)-pyrimidine (nifurpyrimidine).新型硝基呋喃2-氨基-4-甲基-6-(2-乙炔基-5-硝基呋喃基)嘧啶(硝呋嘧啶)在小鼠和大鼠身上的微生物学和药理学评价
Chemotherapy. 1979;25(2):91-5. doi: 10.1159/000237828.
2
[Experimental study of a new nitrofuran. 2-amino-4-methyl-6-(2-ethinyl-5-nitrofuryl)-pyrimidine].一种新型硝基呋喃——2-氨基-4-甲基-6-(2-乙炔基-5-硝基呋喃基)嘧啶的实验研究
G Ital Chemioter. 1978 Jul-Dec;25(2):123-6.
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[Antibacterial activity and toxicity of a new nitrofuran].一种新型硝基呋喃的抗菌活性与毒性
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Nifuratrone, a new nitrofuran: in vitro and in vivo activities.硝呋拉酮,一种新型硝基呋喃:体外和体内活性
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6
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7
Antibacterial activity of some alpha-substituted 2-methyl-5-nitrofurans.一些α-取代的2-甲基-5-硝基呋喃的抗菌活性
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[Chemotherapeutic nitroheterocycles. IV. (1,2)Antimicrobial activity of nitrofurfurylidene, notrothelidene and nitropyrrolmethylene-derivatives of indanones and tetralones].
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