title: Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.
abstract: The synthesis and structure-activity relationships of piperidinylpyrrolopyridines as potent and selective H(1) antagonists are discussed. It was found that the nature of the acid chain bonded to piperidine was a key feature for maintaining both the duration of action in vivo and lack of sedative properties.
authors.affiliation: Almirall Prodesfarma, Research Center, Cardener 68-74, 08024 Barcelona, Spain. sfonquerna@almirall.es
authors.forename: Silvia
authors.initials: S
authors.lastname: Fonquerna
authors.forename: Montse
authors.initials: M
authors.lastname: Miralpeix
authors.forename: Lluís
authors.initials: L
authors.lastname: Pagès
authors.forename: Carles
authors.initials: C
authors.lastname: Puig
authors.forename: Arantxa
authors.initials: A
authors.lastname: Cardús
authors.forename: Francisca
authors.initials: F
authors.lastname: Antón
authors.forename: Dolors
authors.initials: D
authors.lastname: Vilella
authors.forename: Mónica
authors.initials: M
authors.lastname: Aparici
authors.forename: José
authors.initials: J
authors.lastname: Prieto
authors.forename: Graham
authors.initials: G
authors.lastname: Warrellow
authors.forename: Jorge
authors.initials: J
authors.lastname: Beleta
authors.forename: Hamish
authors.initials: H
authors.lastname: Ryder
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001812:Blood-Brain Barrier; D002199:Capillary Permeability; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D006634:Histamine H1 Antagonists; D011725:Pyridines