1,3,4-三取代吡咯烷CCR5受体拮抗剂。第2部分：先导化合物优化，得到具有高效抗HIV活性的选择性口服生物利用化合物。
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
作者信息
Hale J J, Budhu R J, Holson E B, Finke P E, Oates B, Mills S G, MacCoss M, Gould S L, DeMartino J A, Springer M S, Siciliano S, Malkowitz L, Schleif W A, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini E
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2001 Oct 22;11(20):2741-5. doi: 10.1016/s0960-894x(01)00545-5.
Abstract
Investigations of the structure-activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable compounds with the ability to inhibit HIV replication in vitro.
摘要
对1,3,4-三取代吡咯烷类人CCR5受体拮抗剂的构效关系进行研究，得到了具有口服生物利用度且能够在体外抑制HIV复制的化合物。
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