Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.
Novel derivatives of Tolterodine (1) and Oxybutynin (2) have been designed using conformationally restricted azabicyclics as replacement for open-chain amines. The synthesis and structure-activity relationships are presented.
Kaur
Kirandeep
K
Ranbaxy Research Laboratories, New Drug Discovery Research, Department of Medicinal Chemistry, Gurgaon 122 001, Haryana, India.
Aeron
Shelly
S
Bruhaspathy
Miriyala
M
Shetty
Shankar J
SJ
Gupta
Suman
S
Hegde
Laxminarayan H
LH
Silamkoti
Arun D V
AD
Mehta
Anita
A
Chugh
Anita
A
Gupta
Jang B
JB
Sarma
P K S
PK
Kumar
Naresh
N
D000818:Animals; D001559:Benzhydryl Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D003408:Cresols / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D015195:Drug Design; D008333:Mandelic Acids / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D010665:Phenylpropanolamine / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D043585:Receptor, Muscarinic M2 / Q000378:metabolism; D043587:Receptor, Muscarinic M3 / Q000378:metabolism; D013329:Structure-Activity Relationship; D000068737:Tolterodine Tartrate
D001559:Benzhydryl Compounds; D003408:Cresols; D008333:Mandelic Acids; D043585:Receptor, Muscarinic M2; D043587:Receptor, Muscarinic M3; D010665:Phenylpropanolamine; D000068737:Tolterodine Tartrate; C005419:oxybutynin