title: New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
abstract: New histamine H3 receptor antagonists were developed using an acetylene moiety as a replacement for the amide-oxime functionality of verongamine 5. Optimization of receptor binding was performed by following aliphatic Topliss tree guidelines. These new H3 ligands demonstrate excellent blood-brain barrier penetration.
authors.affiliation: Gliatech Inc., Cleveland, Ohio 44122, USA.
authors.forename: S M
authors.initials: SM
authors.lastname: Ali
authors.forename: C E
authors.initials: CE
authors.lastname: Tedford
authors.forename: R
authors.initials: R
authors.lastname: Gregory
authors.forename: S L
authors.initials: SL
authors.lastname: Yates
authors.forename: J G
authors.initials: JG
authors.lastname: Phillips
mesh_terms: D000114:Acetylene / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D015195:Drug Design; D006168:Guinea Pigs; D006321:Heart / Q000294:innervation; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D010091:Oximes / Q000737:chemistry / Q000494:pharmacology*; D018100:Receptors, Histamine H3 / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000378:metabolism; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D006633:Histamine Antagonists; D010091:Oximes; D018100:Receptors, Histamine H3; C086787:verongamine; D014443:Tyrosine; D000114:Acetylene