Article
Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry - 1 Jul 2020
Patel Manoj, Naidu B Narasimhulu, Dicker Ira, Higley Helen, Lin Zeyu, Terry Brian, Protack Tricia, Krystal Mark, Jenkins Susan, Parker Dawn, Panja Chiradeep, Rampulla Richard, Mathur Arvind, Meanwell Nicholas A, Walker Michael A
Abstract excerpt
The design, synthesis and structure-activity relationships associated with a series of bridged tricyclic pyrimidinone carboxamides as potent inhibitors of HIV-1 integrase strand transfer are described. Structural modifications to these molecules were made in order to examine the effect on potency towards wild-type and clinically-relevant resistant viruses. The [3.2.2]-bridged tricyclic system was identified as an...
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