Synthesis and diversity analysis of lead discovery piperazine-2-carboxamide libraries

A Lead Discovery Library of piperazine-2-carboxamide derivatives was produced for general screening. This paper discloses two novel solid phase synthetic routes used to produce 15,000 single compounds via the Irori directed sorting technique. Computational methods such as reagent clustering and libr...

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Bibliographic Details
Published inMolecular diversity Vol. 4; no. 4; pp. 221 - 232
Main Authors Herpin, T F, Morton, G C, Dunn, A K, Fillon, C, Menard, P R, Tang, S Y, Salvino, J M, Labaudinière, R F
Format Journal Article
LanguageEnglish
Published Netherlands Springer Nature B.V 01.01.1998
Subjects
Chemical synthesis
Combinatorial Chemistry Techniques
Pharmacology
Piperazines - chemical synthesis
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Summary:A Lead Discovery Library of piperazine-2-carboxamide derivatives was produced for general screening. This paper discloses two novel solid phase synthetic routes used to produce 15,000 single compounds via the Irori directed sorting technique. Computational methods such as reagent clustering and library profiling were used to maximize reagent diversity and optimize pharmacokinetic parameters. The results of a four center pharmacophore analysis revealed the added diversity gained by using two independent synthetic routes.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1381-1991
1573-501X
DOI:10.1023/A:1009637817478