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Bioorg Med Chem Lett. 2011 May 15;21(10):2890-3. doi: 10.1016/j.bmcl.2011.03.083. Epub 2011 Mar 30.

SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.

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1
Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. gang.zhou@merck.com

Abstract

A novel series of pyridazinone analogs has been developed as potent β-1,3-glucan synthase inhibitors through structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one (1). The effect of changes to the core structure is described in detail. Optimization of the sulfonamide moiety led to the identification of important compounds with much improved systematic exposure while retaining good antifungal activity against the fungal strains Candida glabrata and Candida albicans.

PMID:
21489787
DOI:
10.1016/j.bmcl.2011.03.083
[Indexed for MEDLINE]
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