Shenin Iu D, Belakhov V V, Shatik L I, Arabiĭskiĭ R A
Research Technological Institute of Antibiotics and Medical Enzymes, St. Petersburg.
Antibiot Khimioter. 1998;43(12):8-11.
Reactions of amphotericin B, a polyene macrolide antibiotic, with acyl perfluorides resulted in formation of its N-perfluoroacyl derivatives. Physicochemical and medicobiological properties of the derivatives were studied. The biological study revealed that the acute toxity (LD50) of the derivatives was 2 times as low as that of the starting antibiotic. The derivatives showed high antifungal activity against a great number of the test cultures.
多烯大环内酯类抗生素两性霉素B与酰基过氟化物反应,生成了其N - 全氟酰基衍生物。对这些衍生物的物理化学和药物生物学性质进行了研究。生物学研究表明,这些衍生物的急性毒性(LD50)比起始抗生素低两倍。这些衍生物对大量测试培养物显示出高抗真菌活性。