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.
Novartis Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom.
Vahid
V
Alikhani
David
D
Beer
David
D
Bentley
Ian
I
Bruce
Bernard M
BM
Cuenoud
Robin A
RA
Fairhurst
Peter
P
Gedeck
Sandra
S
Haberthuer
Claire
C
Hayden
Diana
D
Janus
Lynne
L
Jordan
Christine
C
Lewis
Kirsty
K
Smithies
Elke
E
Wissler
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