Novel antifungal agents: triazolopyridines as inhibitors of beta-1,6-glucan synthesis.
Preparations and in vitro antifungal activities of triazolopyridines, imidazopyridines, and a pyrazolopyridine were reported. Among those scaffolds, triazolopyridine was found to be the specific inhibitor of the synthesis of beta-1,6-glucan, an essential component of the fungal cell wall, and to show potent antifungal activities against several Candida species.
Kuroyanagi
Jun-ichi
J
Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd, Edogawa-ku, Tokyo 134-8630, Japan. kuroyanagi.junichi.d5@daiichisankyo.co.jp
Kanai
Kazuo
K
Sugimoto
Yuuichi
Y
Fujisawa
Tetsunori
T
Morita
Chikanori
C
Suzuki
Takashi
T
Kawakami
Katsuhiro
K
Takemura
Makoto
M
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects*; D002177:Candidiasis / Q000188:drug therapy; D004355:Drug Stability; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D008862:Microsomes, Liver / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000187:drug effects; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D047071:beta-Glucans / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D000935:Antifungal Agents; D007093:Imidazoles; D011720:Pyrazoles; D011725:Pyridines; D014230:Triazoles; D047071:beta-Glucans; C064197:beta-1,6-glucan