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 |
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England
Elsevier Ltd
2007
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| Abstract | 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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| AbstractList | 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. 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. |
| Author | Davey, Dave Chou, Yuo-Ling Dunning, Laura Wei, Robert G. Arnaiz, Damian O. Ye, Bin Lu, Shou-Fu Onuffer, James Phillips, Gary Lee, Wheeseong |
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| SubjectTerms | Anti-HIV Agents - chemical synthesis Anti-HIV Agents - chemistry Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry CCR5 CCR5 Receptor Antagonists Cells, Cultured Chemokine receptor antagonists Drug Evaluation, Preclinical Humans Inhibitory Concentration 50 Mitoguazone - analogs & derivatives Structure-Activity Relationship |
| Title | CCR5 receptor antagonists: Discovery and SAR study of guanylhydrazone derivatives |
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