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.
Discovery Chemistry, Sandwich Laboratories, Pfizer Research and Development, Ramsgate Rd, Kent CT2 8DR, UK. lyn.jones@pfizer.com
Lyn H
LH
Jones
Amy
A
Randall
Carolyn
C
Napier
Mike
M
Trevethick
Sasha
S
Sreckovic
Jessica
J
Watson
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