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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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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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creator	TOLLEFSON, M. B VERNIER, W. F HUANG, H.-C FANG PING CHEN REINHARD, E. J BEAUDRY, J KELLER, B. T REITZ, D. B
description	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.
doi_str_mv	10.1016/S0960-894X(99)00683-6
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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
title	A novel class of apical sodium co-dependent bile acid transporter inhibitors : The 2,3-disubstituted-4-phenylquinolines
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