42783-81-3Relevant academic research and scientific papers
Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors
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.
, (2020)
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 advantageous chemotype, with representatives exhibiting excellent antiviral activity against both wild-type viruses and the G140S/Q148H resistant virus that arises in response to therapy with raltegravir and elvitegravir.
