title: Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists.
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.
authors: Discovery Research, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA. mtao@cephalon.com
authors: Ming
authors: M
authors: Tao
authors: Rita
authors: R
authors: Raddatz
authors: Lisa D
authors: LD
authors: Aimone
authors: Robert L
authors: RL
authors: Hudkins
mesh_terms: D000818:Animals; D054828:Histamine H3 Antagonists / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D011724:Pyridazines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D054828:Histamine H3 Antagonists; D011724:Pyridazines; D018100:Receptors, Histamine H3