Prodrugs of CL316243: A selective beta(3)-adrenergic receptor agonist for treating obesity and diabetes

Authors
Sum, FW Gilbert, A Venkatesan, AM Lim, K Wong, V O'Dell, M Francisco, G Chen, Z Grosu, G Baker, J Ellingboe, J Malamas, M Gunawan, I Primeau, J Largis, E Steiner, K
Citation
Fw. Sum et al., Prodrugs of CL316243: A selective beta(3)-adrenergic receptor agonist for treating obesity and diabetes, BIOORG MED, 9(14), 1999, pp. 1921-1926
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
1921 - 1926
Database
ISI
SICI code
0960-894X(19990719)9:14<1921:POCASB>2.0.ZU;2-#
Abstract
CL316243 is a highly selective and potent beta(3)-adrenergic receptor agoni st, and has been shown in rodent models to be an effective agent for treati ng obesity and Type II diabetes. To improve the oral absorption and pharmac okinetic profiles of CL316243, a number of prodrugs have been synthesized a nd evaluated. Several ester-type prodrugs show significant improvements in oral bioavailability in both rodent and primate models, (C) 1999 Elsevier S cience Ltd. All rights reserved.