[Synthesis and antifungal activity of butenafine hydrochloride (KP-363), a new benzylamine antifungal agent].
In screening of new antifungal agents, bis(naphthalenemethyl)amines were found to have more potent antifungal activity than clotrimazole. Studies on their structure-activity relationships indicated that benzylamines had potent antifungal activity. Among them, butenafine hydrochloride (N-p-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride, KP-363) has proved to show the strongest activity. It exhibits a wide spectrum activity in vitro against particularly dermatophytes (87 strains; minimal inhibitory concentration (MIC) range, 0.0015 to 0.05 microgram/ml), and also against Aspergillus (15 strains; MIC range, 0.025 to 0.78 microgram/ml), Cryptococcus neoformans (4 strains; MICs 0.78 and 1.56 micrograms/ml) and yeasts of genus Candida (67 strains; MIC range, 3.13 to greater than 100 micrograms/ml).
Maeda
T
T
Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Tokyo, Japan.
Takase
M
M
Ishibashi
A
A
Yamamoto
T
T
Sasaki
K
K
Arika
T
T
Yokoo
M
M
Amemiya
K
K
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001596:Benzylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D005658:Fungi / Q000187:drug effects*; D006168:Guinea Pigs; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D001596:Benzylamines; D009281:Naphthalenes; C067594:butenafine