Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine

Kirandeep Kaur; Shelly Aeron; Miriyala Bruhaspathy; Shankar J Shetty; Suman Gupta; Laxminarayan H Hegde; Arun D V Silamkoti; Anita Mehta; Anita Chugh; Jang B Gupta; P K S Sarma; Naresh Kumar

doi:10.1016/j.bmcl.2005.02.036

Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2093-6. doi: 10.1016/j.bmcl.2005.02.036.

Authors

Kirandeep Kaur¹, Shelly Aeron, Miriyala Bruhaspathy, Shankar J Shetty, Suman Gupta, Laxminarayan H Hegde, Arun D V Silamkoti, Anita Mehta, Anita Chugh, Jang B Gupta, P K S Sarma, Naresh Kumar

Affiliation

¹ Ranbaxy Research Laboratories, New Drug Discovery Research, Department of Medicinal Chemistry, Gurgaon 122 001, Haryana, India.

PMID: 15808475
DOI: 10.1016/j.bmcl.2005.02.036

Abstract

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.

MeSH terms

Animals
Benzhydryl Compounds / chemical synthesis*
Benzhydryl Compounds / metabolism
Benzhydryl Compounds / pharmacology*
Binding Sites / drug effects
Cresols / chemical synthesis*
Cresols / metabolism
Cresols / pharmacology*
Drug Design*
Mandelic Acids / chemical synthesis*
Mandelic Acids / metabolism
Mandelic Acids / pharmacology*
Phenylpropanolamine / chemical synthesis*
Phenylpropanolamine / metabolism
Phenylpropanolamine / pharmacology*
Rats
Receptor, Muscarinic M2 / metabolism
Receptor, Muscarinic M3 / metabolism
Structure-Activity Relationship
Tolterodine Tartrate

Substances

Benzhydryl Compounds
Cresols
Mandelic Acids
Receptor, Muscarinic M2
Receptor, Muscarinic M3
Phenylpropanolamine
Tolterodine Tartrate
oxybutynin