A novel class of apical sodium co-dependent bile acid transporter inhibitors : The 2,3-disubstituted-4-phenylquinolines

A series of 2,3-disubstituted-4-phenylquinolines were prepared and were found to inhibit the apical sodium co-dependent bile acid transporter (ASBT). Alkyl and ester substitution at the 3-position showed comparable activities while substitution at the 2-position was much more sensitive to the nature...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-02, Vol.10 (3), p.277-279
Main Authors: TOLLEFSON, M. B, VERNIER, W. F, HUANG, H.-C, FANG PING CHEN, REINHARD, E. J, BEAUDRY, J, KELLER, B. T, REITZ, D. B
Format: Article
Language:English
Subjects:
Biological and medical sciences
Carrier Proteins - antagonists & inhibitors
Fundamental and applied biological sciences. Psychology
Hydroxysteroid Dehydrogenases
Intestine. Mesentery
Medical sciences
Membrane Glycoproteins
Miscellaneous
Molecular Structure
Pharmacology. Drug treatments
Quinolines - chemistry
Quinolines - pharmacology
Sodium - pharmacology
Vertebrates: digestive system
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Summary:A series of 2,3-disubstituted-4-phenylquinolines were prepared and were found to inhibit the apical sodium co-dependent bile acid transporter (ASBT). Alkyl and ester substitution at the 3-position showed comparable activities while substitution at the 2-position was much more sensitive to the nature of the substituent. The synthesis and in vitro potency data are presented for this novel class of compounds.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00683-6