CCR5 receptor antagonists: Discovery and SAR study of guanylhydrazone derivatives
High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Modifications of the guanylhydrazone resulted in the discovery of novel CCR5 antagonists. High throughput screening (HTS) led to the identifica...
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Published in | Bioorganic & medicinal chemistry letters Vol. 17; no. 1; pp. 231 - 234 |
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Main Authors | , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
England
Elsevier Ltd
2007
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Subjects | |
Online Access | Get full text |
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Summary: | High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Modifications of the guanylhydrazone resulted in the discovery of novel CCR5 antagonists.
High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Initial modifications of the guanylhydrazone series indicated that substitution of the benzyl group at the para-position was well tolerated. Substitution at the 5-position of the central phenyl ring was critical for potency. Replacement of the guanylhydrazone group led to the discovery of a novel series of CCR5 antagonists. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2006.09.052 |