期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 17, 页码 5205-5208出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.020
关键词
CXCR3 receptor antagonists; Piperazinyl-piperidine; Combinatorial chemistry; Solid-phase synthesis; Chemokine
High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesized via solid and solution phase methods to probe the influence of structure on the CXCR3 binding of these molecules. Various functional groups were found to contribute to the overall potency and essential molecular features were identified. (C) 2009 Elsevier Ltd. All rights reserved.
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