Discovery of novel indazole-linked triazoles as antifungal agents.

Abstract

The in vitro and in vivo activities of a series of (2R,3R)-2-(2,4-difluorophenyl)-3-(substituted indazol-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol as potential antifungal agents are described. In particular, the analog 12j having 5-bromo substitution on the indazole ring exhibited significant antifungal activity against a variety of fungal cultures (Candida spp. and Aspergillus spp.). In addition, oral administration of 12j showed its excellent efficacy against Candida albicans in a murine infection model and the significantly improved survival rates of the infected mice.

• Authors: Joon Seok Park, Kyung A Yu, Tae Hee Kang, Sunghoon Kim, Young-Ger Suh
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 12 Pg. 3486-90 (Jun 15 2007) ISSN: 0960-894X [Print] England
• PMID: 17433670 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antifungal Agents
• Indazoles
• Triazoles

Topics

• Administration, Oral
• Animals
• Antifungal Agents (chemical synthesis, pharmacology, therapeutic use)
• Aspergillus (drug effects, growth & development)
• Candida (drug effects, growth & development)
• Disease Models, Animal
• Indazoles (chemical synthesis, pharmacology, therapeutic use)
• Mice
• Microbial Sensitivity Tests
• Rats
• Stereoisomerism
• Triazoles (chemical synthesis, pharmacology, therapeutic use)