Chemical and Pharmaceutical Bulletin p. 60 - 64 (2000)
Update date:2022-07-30
Topics:
Hori, Kimihiko
Sakaguchi, Akira
Kudoh, Michinari
Ishida, Koichi
Aoyama, Yuri
Yoshida, Yuzo
Fungicidal activity of widely used imidazole antifungal drugs in topical applications is not so strong in spite of their potent fungistatic activities against dermatophytes and pathogenic yeasts. In order to improve fungicidal activity of imidazole antifungal agents, a series of novel imidazole derivatives having a hydrophobic substituent derived from isoprenoid were synthesized. The efficacy of these compounds was evaluated with respect to direct cell-membrane damaging activity, ergosterol biosynthesis inhibition, minimum growth-inhibitory concentration (MIC) and therapeutic effect for experimental dermatophytosis of guinea pigs. Among the newly synthesized compounds, the geranyl derivative named AFK-108 (2a) showed the highest in vivo fungicidal activity with both cell membrane damaging activity and ergosterol biosynthesis inhibition in vitro.
View MoreContact:852-27701081
Address:Room 2509, New Tech Plaza, 34 Tai Yau St., San Po Kong, HK
website:http://www.aecochemical.com
Contact:+86-592 599 8717
Address:No 611 Sishui Road,Huli
HAINAN JINYING IMPORT AND EXPORT CO. LTD
Contact:+86-898-32875423
Address:A SECTION 19TH FL, TIMES SQUARE, NO.2 GUO MAO AVENUE HAIKOU, HAINAN, P. R. OF CHINA
AllyChem Co., Ltd., Dalian, China（BBChem）
Contact:+86-411-62313318/62313328
Address:No.5 of Jinbin Road, Jinzhou New District, Dalian City, Liaoning Province, P.R.China
Contact:+33-5-34012600
Address:28 ZA des Pignès
Doi:10.1016/j.tet.2011.10.099
(2012)Doi:10.1016/j.tetlet.2011.10.117
(2012)Doi:10.1055/s-0030-1260244
(2011)Doi:10.1002/anie.201814197
(2019)Doi:10.1055/s-0030-1260215
(2011)Doi:10.1039/c2dt11862a
(2012)
