Malabarba A, Pallanza R, Berti M, Cavalleri B
Merrell Dow Research Institute, Lepetit Research Center, Varese, Italy.
J Antibiot (Tokyo). 1990 Sep;43(9):1089-97. doi: 10.7164/antibiotics.43.1089.
A series of basic carboxamides of actagardine (1), a lantibiotic possessing good antistreptococcal activity, were synthetized. Some physico-chemical characteristics, in particular charge and lipophilicity, that influence water solubility were determined. The in vitro and in vivo activity was evaluated. The monocarboxamides were generally more active than actagardine against selected Gram-positive bacteria. The 3,3-dimethylamino-1-propylamide hydrochloride (4) showed good water solubility, bactericidal action and favourable antibacterial activity and it appears to be a suitable drug for further investigation.
合成了一系列具有良好抗链球菌活性的羊毛硫抗生素阿他加定（1）的碱性羧酰胺。测定了一些影响水溶性的物理化学特性，特别是电荷和亲脂性。评估了其体外和体内活性。单羧酰胺对选定的革兰氏阳性菌通常比阿他加定更具活性。3,3-二甲基氨基-1-丙酰胺盐酸盐（4）表现出良好的水溶性、杀菌作用和有利的抗菌活性，似乎是一种适合进一步研究的药物。
