Exploration of a new series of CCR5 antagonists: Multi-dimensional optimization of a sub-series containing N-substituted pyrazoles

…, A Jekle, G Heilek, C Ji, P Berry, DM Rotstein

文献索引：Lemoine, Remy C.; Petersen, Ann C.; Setti, Lina; Jekle, Andreas; Heilek, Gabrielle; Derosier, Andre; Ji, Changhua; Berry, Pamela; Rotstein, David M. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 16 p. 4753 - 4756

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被引用次数: 6

摘要

We recently described a new series of CCR5 antagonists with compounds 1 and 3 being two representatives. 2 This series contains the four pharmacophores found in most of the series reported in the literature: a tertiary basic amine, two hydrophobic groups in the western portion of the molecule (henceforth referred to as the tail), including the tail hydrophobe 1, and an (hetero)aryl in the eastern portion of the molecule (the head). We describe herein, part of our SAR focusing ...