Welcome to LookChem.com Sign In|Join Free

Article Doi

Structure-activity relationships of a new antifungal imidazole, AFK-108, and related compounds

DOI: 10.1248/cpb.48.60

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 60 - 64 (2000)

Update date:2022-07-30

Topics:

Authors:

Hori, KimihikoHori, Kimihiko

Sakaguchi, AkiraSakaguchi, Akira

Kudoh, MichinariKudoh, Michinari

Ishida, KoichiIshida, Koichi

Aoyama, YuriAoyama, Yuri

Yoshida, YuzoYoshida, Yuzo

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1248/cpb.48.60

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 More

Full text of DOI:10.1248/cpb.48.60

NII-Electronic Library Service  
NII-Electronic Library Service  
NII-Electronic Library Service  
NII-Electronic Library Service  
NII-Electronic Library Service  

Products guided by the article

Product name:1-[2-(2,4-dichlorophenyl)-2-{[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]oxy}ethyl]-1H-imidazole

Cas No:135330-86-8

135330-86-8

R&D Labs maybe for 135330-86-8

Relevant to this article

Hot Product