A structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one 1 has resulted in the identification of 2-(3,5-difluorophenyl)-4-(3-fluorocyclopentyloxy)-5-[4-(isopropylsulfonyl)piperazin-1-yl]-pyridazin-3(2H)-one 11c as a β-1,3-glucan synthase inhibitor. Compound 11c exhibited significant efficacy in an in vivo mouse model of Candida glabrata infection.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2011.01.058 | DOI Listing |
Publication Analysis
Top Keywords
structure-activity relationship
8
synthesis structure-activity
4
relationship pyridazinones
4
pyridazinones glucan
4
glucan synthase
4
synthase inhibitors
4
inhibitors structure-activity
4
relationship study
4
study lead
4
lead 5-[4-benzylsulfonylpiperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-32h-one
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!