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ChemInform Abstract: Design and Synthesis of 1,4-Diazabicyclo[4.3.0]nonane Peptidomimetic Endothelin Antagonists.

✍ Scribed by Ming Fai Chan; Bore G. Raju; Adam Kois; Jay I. Varughese; Kottayil I. Varughese; Vitukudi N. Balaji

Publisher: John Wiley and Sons
Year: 2010
Weight: 36 KB
Volume: 30
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199926162

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✦ Synopsis

Design and Synthesis of 1,4-Diazabicyclo[4.3.0]nonane Peptidomimetic Endothelin Antagonists.

-Four peptidomimetics such as (XI) are synthesized in order to examine the effect of the carboxyl group stereochemistry on the biological activity. The structures of the peptidomimetics are based on the peptide endothelin antagonists BQ-123 and FR139317. Only isomer (XI) shows moderate affinity for the ET A receptor. Thus, the framework is relatively rigid and may be a suitable scaffold for other types of peptidomimetics. -(CHAN,

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