Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses
文献类型：期刊论文
| 作者 | LE GIANG ; VANDEGRAAFF NICK ; RHODES DAVID I ; JONES ERIC D ; COATES JONATHAN A V ; Lv L(吕龙) ; LI XINMING ; YU CHANGJIANG ; FENG XIAO ; DEADMAN JOHN J |
| 刊名 | Bioorg. Med. Chem. Lett.
 |
| 出版日期 | 2010 |
| 卷号 | 20期号:17页码:5013-5018 |
| ISSN号 | 0960-894X |
| 其他题名 | Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses |
| 通讯作者 | LE GIANG ; DEADMAN JOHN J |
| 英文摘要 | A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against wild-type virus were successfully maintained at single digit nanomolar level with a wide range of substitutions. However, inclusion of nitrogen-based cyclic substitutions was crucial for achieving potency against mutant viruses. Several compounds with excellent activities against wild-type virus as well as against the viruses with the mutations Q148H/G140S or N155H/E92Q were reported. (C) 2010 Elsevier Ltd. All rights reserved. |
| 学科主题 | 氟化学 ; 生命有机化学 |
| 收录类别 | SCI |
| 原文出处 | http://dx.doi.org/10.1016/j.bmcl.2010.07.041 |
| 语种 | 英语 |
| WOS记录号 | WOS:000281247000007 |
| 公开日期 | 2013-02-25 |
| 源URL | [http://202.127.28.38/handle/331003/19233]  |
| 专题 | 上海有机化学研究所_中科院有机氟化学重点实验室 |
| 推荐引用方式 GB/T 7714 | LE GIANG,VANDEGRAAFF NICK,RHODES DAVID I,et al. Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses[J]. Bioorg. Med. Chem. Lett.,2010,20(17):5013-5018. |
| APA | LE GIANG.,VANDEGRAAFF NICK.,RHODES DAVID I.,JONES ERIC D.,COATES JONATHAN A V.,...&DEADMAN JOHN J.(2010).Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses.Bioorg. Med. Chem. Lett.,20(17),5013-5018. |
| MLA | LE GIANG,et al."Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses".Bioorg. Med. Chem. Lett. 20.17(2010):5013-5018. |
入库方式： OAI收割
来源：上海有机化学研究所
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