✦ LIBER ✦

The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317

✍ Scribed by Nicholas K. Terrett; Dejan Bojanic; David Brown; Peter J. Bungay; Mark Gardner; David W. Gordon; Carolyn J. Mayers; John Steele

Book ID: 103982915
Publisher: Elsevier Science
Year: 1995
Tongue: English
Weight: 327 KB
Volume: 5
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00144-i

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✦ Synopsis

A combinatorial library of 30,752 compounds has been synthesised from a set of 32 natural and unnatural amino acids. The library was designed to include the known endothelin antagonist, FR-139,317, as a positive control, and this and a number of close analogues were shown to be the most potent compounds. Thus, combinatorial libraries may be used both to discover leads and rapidly explore SAR.