CCR5 receptor antagonists: Discovery and SAR study of guanylhydrazone derivatives
Copyright policy )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. 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.
Mitoguazone, Anti-HIV Agents, Anti-Inflammatory Agents, Non-Steroidal, Drug Evaluation, Preclinical, Inhibitory Concentration 50, Structure-Activity Relationship, CCR5 Receptor Antagonists, Humans, Cells, Cultured
Mitoguazone, Anti-HIV Agents, Anti-Inflammatory Agents, Non-Steroidal, Drug Evaluation, Preclinical, Inhibitory Concentration 50, Structure-Activity Relationship, CCR5 Receptor Antagonists, Humans, Cells, Cultured
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