期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 14, 页码 6850-6859出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.05.067
关键词
neurokinin; NK1 receptor; substance P; synthesis; amide derivatives
The substituent in position 2 of the quinoline nucleus of NK1 receptor ligands 5 has been constrained into different five-membered heterocyclic moieties in order to obtain information on the binding site pocket interacting with this apparently critical portion of ligands 5. This structure-affinity relationship study led to the discovery of novel tricyclic NK1 receptor ligands 6 showing affinity in the nanomolar range to the sub-micromolar one. The systematic structure variation suggests that electronic features of the tricyclic moiety play a role in modulating the interaction of these amide derivatives with their receptor. (c) 2008 Elsevier Ltd. All rights reserved.
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