Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
The synthesis of a series of long-chain formoterol analogues in which the terminal ether residue of the beta-phenethyl-amino-substituent has been extended beyond the methyl ether residue present in the parent compound are described. Evaluation of these analogues as beta(2)-adrenoceptor agonists was used to provide an insight into the factors controlling the magnitude and duration of receptor activation.
Alikhani
Vahid
V
Novartis Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom.
Beer
David
D
Bentley
David
D
Bruce
Ian
I
Cuenoud
Bernard M
BM
Fairhurst
Robin A
RA
Gedeck
Peter
P
Haberthuer
Sandra
S
Hayden
Claire
C
Janus
Diana
D
Jordan
Lynne
L
Lewis
Christine
C
Smithies
Kirsty
K
Wissler
Elke
E
D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000420:Albuterol / Q000031:analogs & derivatives* / Q000737:chemistry; D000818:Animals; D004983:Ethanolamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000068759:Formoterol Fumarate; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D000068299:Salmeterol Xinafoate; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013997:Time Factors
D058666:Adrenergic beta-2 Receptor Agonists; D000318:Adrenergic beta-Agonists; D004983:Ethanolamines; D000068299:Salmeterol Xinafoate; D000420:Albuterol; D000068759:Formoterol Fumarate