Configurationally restricted bismacrocyclic CXCR4 receptor antagonists.
نویسندگان
چکیده
A zinc(II) containing configurationally restricted analogue of bismacrocyclic cyclam-type CXCR4 chemokine receptor antagonists has been synthesized and shown to adopt only one configuration in solution. The single crystal X-ray structure reveals favorable binding to acetate via a bidentate chelation that can be related to the proposed interaction with aspartate on the receptor protein surface. The zinc(II) complex is highly active against HIV infection in vitro.
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ورودعنوان ژورنال:
- Journal of medicinal chemistry
دوره 49 21 شماره
صفحات -
تاریخ انتشار 2006