Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication

…, C Smith, T Wilson, D Veale, H Yee, J Crawford…

文献索引：Skerlj, Renato; Bridger, Gary; McEachern, Ernie; Harwig, Curtis; Smith, Chris; Wilson, Trevor; Veale, Duane; Yee, Helen; Crawford, Jason; Skupinska, Krystyna; Wauthy, Rossana; Yang, Wen; Zhu, Yongbao; Bogucki, David; Di Fluri, Maria; Langille, Jonathon; Huskens, Dana; De Clercq, Erik; Schols, Dominique Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 262 - 266

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被引用次数: 24

摘要

An early lead from the AMD070 program was optimized and a structure–activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca2+ flux inhibition that displayed good pharmacokinetics in rat and dog.