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ChemInform Abstract: Benzofuran Derivatives as ETA-Selective, Non-Peptide Endothelin Antagonists.

โœ Scribed by J. S. KALTENBRONN; J. III QUIN; B. R. REISDORPH; S. KLUTCHKO; E. E. REYNOLDS; K. M. WELCH; M. A. FLYNN; A. M. DOHERTY

Publisher
John Wiley and Sons
Year
2010
Weight
33 KB
Volume
28
Category
Article
ISSN
0931-7597

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โœฆ Synopsis

Benzofuran Derivatives as ETA-Selective, Non-Peptide Endothelin Antagonists.

-A series of benzofuran derivatives is prepared where the ether moiety, the 3-methyl group, and the 2-carboxy function are varied sequentially. Compounds such as (VI) show 2-to 16-fold selective binding to the ETA receptor in the micromolar range, and two derivatives from this series cf. (VIc) and (VId), exhibit ETA antagonist activity. All modifications of the carboxyl group lead to inactive compounds except analogue (IX), which shows activity comparable to that of the carboxylic acid derivatives.

-(KALTENBRONN,

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ChemInform Abstract: Benzofuro[3,2-b]pyr
ChemInform Abstract: Benzofuro[3,2-b]pyridines as Mixed ETA/ETB and Selective ETB Endothelin Receptor Antagonists.
โœ Werner W. K. R. Mederski; Mathias Osswald; Dieter Dorsch; Maria Christadler; Cla ๐Ÿ“‚ Article ๐Ÿ“… 2010 ๐Ÿ› John Wiley and Sons โš– 35 KB ๐Ÿ‘ 1 views

Benzofuro[3, pyridines as Mixed ET A /ET B and Selective ET B Endothelin Receptor Antagonists. -A series of title compounds, e.g. (IX), is prepared and tested for the desired endothelin receptor antagonistic activity. The general synthetic method is described for compound (VIII) showing moderate a