Terekhov V I, Pavlov P A
Antibiot Khimioter. 1995 Apr;40(4):34-6.
A new nitrofuran, N-(5-nitrofurfurilidene)-5-nitrofuran-2-(N'-acetyl)carboxamidra zone designated as PAP-49 was synthesized. With the method of two-fold serial dilutions in the Hottinger's broth it was demonstrated that by its antimicrobial activity against cocci and enterobacteria PAP-49 was not inferior and in some cases it was even superior to such antibiotics and chemical drugs as benzylpenicillin, streptomycin, tetracycline, chloramphenicol, erythromycin, gentamicin, nitoxolin and furazolidone. The further study of the antibacterial properties of the new nitrofuran with the use of 101 strains of 16 bacterial species showed that its MICs for gram positive and gram negative bacteria were 0.03-3.13 and 0.78-125.0 micrograms/ml respectively. Combination of PAP-49 in the subbacteriostatic concentrations with other antimicrobial agents provided a 2-8-fold increase in the antimicrobial effect. The highest synergism was observed when nitrofuran was used in combination with aminoglycosides, benzylpenicillin or levomycetin. The primary screening revealed that PAP-49 belongs to the group of low toxic substances. Its LD50 after the oral administration to albino mice was 4631.9 mg/kg. The compound did not practically cumulate in the animal organism.
合成了一种新的硝基呋喃,即N-(5-硝基糠叉基)-5-硝基呋喃-2-(N'-乙酰基)羧酰胺腙,命名为PAP-49。采用在霍廷格肉汤中两倍系列稀释法表明,PAP-49对球菌和肠道杆菌的抗菌活性不低于,在某些情况下甚至优于苄青霉素、链霉素、四环素、氯霉素、红霉素、庆大霉素、硝羟喹啉和呋喃唑酮等抗生素和化学药物。使用16种细菌的101株菌株对这种新硝基呋喃的抗菌特性进行的进一步研究表明,其对革兰氏阳性菌和革兰氏阴性菌的最低抑菌浓度分别为0.03 - 3.13微克/毫升和0.78 - 125.0微克/毫升。PAP-49在亚抑菌浓度下与其他抗菌剂联合使用可使抗菌效果提高2至8倍。当硝基呋喃与氨基糖苷类、苄青霉素或氯霉素联合使用时,观察到最高的协同作用。初步筛选表明,PAP-49属于低毒物质组。对白化小鼠口服给药后其半数致死量为4631.9毫克/千克。该化合物在动物体内几乎不蓄积。