Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors

Makonen Belema; Amy Bunker; Van N Nguyen; Francis Beaulieu; Carl Ouellet; Yuping Qiu; Yunhui Zhang; Alain Martel; James R Burke; Kim W McIntyre; Mark A Pattoli; Connie Daloisio; Kathleen M Gillooly; Wendy J Clarke; Patrick J Brassil; F Chris Zusi; Dolatrai M Vyas

doi:10.1016/j.bmcl.2007.05.031

Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. doi: 10.1016/j.bmcl.2007.05.031. Epub 2007 May 16.

Authors

Makonen Belema¹, Amy Bunker, Van N Nguyen, Francis Beaulieu, Carl Ouellet, Yuping Qiu, Yunhui Zhang, Alain Martel, James R Burke, Kim W McIntyre, Mark A Pattoli, Connie Daloisio, Kathleen M Gillooly, Wendy J Clarke, Patrick J Brassil, F Chris Zusi, Dolatrai M Vyas

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. makonen.belema@bms.com

PMID: 17540562
DOI: 10.1016/j.bmcl.2007.05.031

Abstract

The identification of a potent series of IKK-beta selective inhibitors based on an imidazothienopyrazine template and the oral efficacy of one such analog (22j) in the LPS-induced TNF-alpha release mouse model are described.

MeSH terms

Animals
Cells, Cultured
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Humans
I-kappa B Kinase / antagonists & inhibitors*
Mice
Pyrazines / chemical synthesis
Pyrazines / chemistry*
Pyrazines / pharmacology*
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Pyrazines
I-kappa B Kinase