Synthesis and evaluation of novel antifungal agents-quinoline and pyridine amide derivatives.
Quinoline amide, azaindole amide and pyridine amides were synthesized and tested for in vitro antifungal activity against fungi. These synthesized amides have potent antifungal activity against Candida albicans and Aspergillus fumigatus. Our results suggest that hetero ring amides may be potent antifungal agents that operate by inhibiting the function of Gwt1 protein in the GPI biosynthetic pathway.
Nakamoto
Kazutaka
K
Discovery Research Laboratories, Eisai Co., Ltd, Tsukuba-shi, Ibaraki 300-2635, Japan. k3-nakamoto@hhc.eisai.co.jp
Tsukada
Itaru
I
Tanaka
Keigo
K
Matsukura
Masayuki
M
Haneda
Toru
T
Inoue
Satoshi
S
Murai
Norio
N
Abe
Shinya
S
Ueda
Norihiro
N
Miyazaki
Mamiko
M
Watanabe
Naoaki
N
Asada
Makoto
M
Yoshimatsu
Kentaro
K
Hata
Katsura
K
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001232:Aspergillus fumigatus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D005656:Fungal Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D011725:Pyridines / Q000737:chemistry*; D011804:Quinolines / Q000737:chemistry*
D000577:Amides; D000935:Antifungal Agents; D005656:Fungal Proteins; D011725:Pyridines; D011804:Quinolines; C037219:quinoline; C023666:pyridine