Tsutsumi S, Gidoh M
Nihon Rai Gakkai Zasshi. 1989 Oct-Dec;58(4):250-8. doi: 10.5025/hansen1977.58.250.
In order to develop a novel drug for antileprosy chemotherapy, the inhibitory effects of three synthesized compounds, a supplied antituberculous one and three quinolone carboxylic acids were examined on the growth of leprosy bacilli inoculated into the footpads of nude mice. Amongst them, a new quinolone carboxylic acid, AT-4140 whose chemical structure was 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(cis-3, 5-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid strongly inhibited the growth of leprosy bacilli at doses of 15 and 30 mg/kg. Whereas, the effect of Ofloxacin used as a positive control was limited at the same doses.
为开发一种用于麻风病化疗的新型药物,研究了三种合成化合物、一种提供的抗结核药物以及三种喹诺酮羧酸对接种于裸鼠足垫的麻风杆菌生长的抑制作用。其中,一种化学结构为5-氨基-1-环丙基-6,8-二氟-1,4-二氢-7-(顺式-3,5-二甲基-1-哌嗪基)-4-氧代喹啉-3-羧酸的新型喹诺酮羧酸AT-4140,在15和30mg/kg剂量时能强烈抑制麻风杆菌生长。而作为阳性对照的氧氟沙星在相同剂量下作用有限。