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Bioorg Med Chem Lett. 2011 Aug 15;21(16):4762-7. doi: 10.1016/j.bmcl.2011.06.067. Epub 2011 Jun 29.

Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors.

Author information

1
Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, PO Box 776, Spring House, PA 19477, United States. xzhang5@its.jnj.com

Abstract

A series of indazoles have been discovered as KHK inhibitors from a pyrazole hit identified through fragment-based drug discovery (FBDD). The optimization process guided by both X-ray crystallography and solution activity resulted in lead-like compounds with good pharmaceutical properties.

PMID:
21767952
DOI:
10.1016/j.bmcl.2011.06.067
[Indexed for MEDLINE]

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