| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374611 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
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.
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Related Topics
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Authors
Giang Le, Nick Vandegraaff, David I. Rhodes, Eric D. Jones, Jonathan A.V. Coates, Long Lu, Xinming Li, Changjiang Yu, Xiao Feng, John J. Deadman,