Bioorg Med Chem Lett. 2011 Oct 15;21(20):6126-30. doi: 10.1016/j.bmcl.2011.08.045. Epub 2011 Aug 19.

Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.

Tao M, Raddatz R, Aimone LD, Hudkins RL.

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Discovery Research, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA. mtao@cephalon.com

Abstract

Three series of novel 4,5-fused pyridazinones were synthesized as histamine H(3) receptor antagonists. The 2,5,6,7-tetrahydrocyclopenta[d]pyridazin-1-one 5q and 5,6,7,8-tetrahydro-2H-phthalazin-1-one 5u displayed high affinity at both rat and human H(3) receptors, and showed potent antagonist and full inverse agonist activity in functional assays.

PMID:: 21906941; [PubMed - indexed for MEDLINE]

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Synthesis and structure-activity relationships of 4,5-fused pyridazinones as his...
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.
Bioorg Med Chem Lett. 2011 Oct 15 ;21(20):6126-30. doi: 10.1016/j.bmcl.2011.08.045. Epub 2011 Aug 19 .

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