| Literature DB >> 20685117 |
Giang Le1, Nick Vandegraaff, David I Rhodes, Eric D Jones, Jonathan A V Coates, Long Lu, Xinming Li, Changjiang Yu, Xiao Feng, John J Deadman.
Abstract
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. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20685117 DOI： 10.1016/j.bmcl.2010.07.041
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823