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Updated: Jun 10, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses
Giang Le1, Nick Vandegraaff, David I Rhodes
1Avexa Ltd, 576 Swan Street, Richmond, Victoria 3121, Australia.
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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