Studies on the development of novel anti-leprous chemotherapeutics using nude mice with special reference to a new quinolone carboxylic acid, AT-4140.

Abstract

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.