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

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.