title: Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
abstract: Starting with the molecular scaffold of the DA(2)/β(2) dual agonist sibenadet (Viozan™), a number of molecular changes were incorporated, which were designed to increase the potency and selectivity of the target molecule, and improve its pharmacokinetics. Through this process a novel, high potency, full β(2)-agonist with high selectivity and long duration capable of being dosed once daily has been discovered.
authors: Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, Leicestershire, UK. steve.connolly@astrazeneca.com
authors: Stephen
authors: S
authors: Connolly
authors: Lilian
authors: L
authors: Alcaraz
authors: Andrew
authors: A
authors: Bailey
authors: Elaine
authors: E
authors: Cadogan
authors: Jadeen
authors: J
authors: Christie
authors: Anthony R
authors: AR
authors: Cook
authors: Adrian J
authors: AJ
authors: Fisher
authors: Stephen
authors: S
authors: Hill
authors: Alexander
authors: A
authors: Humphries
authors: Anthony H
authors: AH
authors: Ingall
authors: Zoe
authors: Z
authors: Kane
authors: Stuart
authors: S
authors: Paine
authors: Garry
authors: G
authors: Pairaudeau
authors: Michael J
authors: MJ
authors: Stocks
authors: Alan
authors: A
authors: Young
mesh_terms: D058666:Adrenergic beta-2 Receptor Agonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D001993:Bronchodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D018343:Receptors, Adrenergic, beta-2 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D058666:Adrenergic beta-2 Receptor Agonists; D001993:Bronchodilator Agents; D018343:Receptors, Adrenergic, beta-2; D013844:Thiazoles; C116267:sibenadet