Design and synthesis of a fluorescent muscarinic antagonist.
The design and concise synthesis of a fluorescent tolterodine-BODIPY (boron dipyrromethene) conjugate is described which possesses potent antimuscarinic activity. This derivative illustrates proof-of-concept for the preparation of other useful fluorophoric antimuscarinic agents which have potential utility in receptor occupancy studies and high throughput screens.
Jones
Lyn H
LH
Discovery Chemistry, Sandwich Laboratories, Pfizer Research and Development, Ramsgate Rd, Kent CT2 8DR, UK. lyn.jones@pfizer.com
Randall
Amy
A
Napier
Carolyn
C
Trevethick
Mike
M
Sreckovic
Sasha
S
Watson
Jessica
J
D002855:Chromatography, Thin Layer; D005456:Fluorescent Dyes / Q000737:chemistry*; D006207:Half-Life; D009682:Magnetic Resonance Spectroscopy; D018727:Muscarinic Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
D005456:Fluorescent Dyes; D018727:Muscarinic Antagonists