当前位置：
X-MOL 学术
›
Bioorg. Med. Chem. Lett.
›
论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-06-26 , DOI: 10.1016/j.bmcl.2020.127367 Dane J Clausen 1 , Jian Liu 1 , Wensheng Yu 1 , Joseph L Duffy 1 , Christine C Chung 1 , Robert W Myers 1 , Daniel J Klein 2 , James Fells 2 , Kate Holloway 2 , Jin Wu 1 , Guoxin Wu 2 , Bonnie J Howell 2 , Richard J O Barnard 2 , Joseph Kozlowski 1
中文翻译：
选择性HDAC抑制剂的开发旨在重新激活HIV潜伏库。
更新日期：2020-07-05
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-06-26 , DOI: 10.1016/j.bmcl.2020.127367 Dane J Clausen 1 , Jian Liu 1 , Wensheng Yu 1 , Joseph L Duffy 1 , Christine C Chung 1 , Robert W Myers 1 , Daniel J Klein 2 , James Fells 2 , Kate Holloway 2 , Jin Wu 1 , Guoxin Wu 2 , Bonnie J Howell 2 , Richard J O Barnard 2 , Joseph Kozlowski 1
Affiliation
|
The synthesis and SAR development of a trisubstituted imidazole HDAC inhibitor is described. The compounds were synthesized with high diastereocontrol by leveraging Ellman sulfinyl imine chemistry. Structural elucidation provided insight into binding mode and supported design rational. Pharmacokinetic properties of lead compounds were determined.
中文翻译：
选择性HDAC抑制剂的开发旨在重新激活HIV潜伏库。
描述了三取代的咪唑HDAC抑制剂的合成和SAR发展。通过利用埃尔曼亚磺酰基亚胺化学，以高度非对映体控制合成了这些化合物。结构解析提供了对绑定模式的洞察力并支持了设计合理性。测定了铅化合物的药代动力学性质。
京公网安备 11010802027423号