Abstract
11-jodo-10-undecynoic acid (K-4172) was synthesised in our laboratory from 10-undecynoic acid reacting with iodine in presence of alkaline hydroxide. Fungistatic and bacteriostatic activities of K-4172 were examined. It showed significant antifungal activities, especially against Trichophytons and Crytococcus neoformans, but it had weak antibacterial activities.
In in vivo test by experimental trichophytosis on guineapigs, it showed also significant therapeutic activities at the concentration of 0.5% in alcohol solution. It is very interest that in the in vivo test 0.5% tincture of K-4172 was more effective when it was applied in combination with 10% of 2, 4, 6-tribromophenyl caproate.
Interperitoneal and oral LD50 of K-4172 dissolved in olive oil were 132 and 225mg/Kg respectively and intraperitoneal LD50 of its sodium salt was 134mg/Kg. Chronic toxicity test of K-4172 on mice and rat showed both almost no side effect when it was admidistrated intraperitoneally and orally. The authers persume from these data that K-4172 is safely available for treatment of human trichophytosis.
