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Identification of spirocyclic or phosphate substituted quinolizine derivatives as novel HIV-1 integrase inhibitors: A patent evaluation of WO2016094197A1, WO2016094198A1 and WO2016154527A1.

Identification of spirocyclic or phosphate substituted quinolizine derivatives as novel HIV-1 integrase inhibitors: A patent evaluation of WO2016094197A1, WO2016094198A1 and WO2016154527A1.
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Cheng X, Gao P, Sun L, Tian Y, Zhan P, Liu X,


Cheng X, Gao P, Sun L, Tian Y, Zhan P, Liu X, (click to view)

Cheng X, Gao P, Sun L, Tian Y, Zhan P, Liu X,

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Expert opinion on therapeutic patents 2017 07 27() doi 10.1080/13543776.2017.1360283

Abstract
INTRODUCTION
Highly active antiretroviral therapy (HAART) has been widely adopted to control the HIV-1 infection successfully. HIV-1 integrase (IN) inhibitors are primary drugs in HAART regimens targeting integration step in the HIV-1 life cycle. However, due to the emergence of viral resistance and cross-resistance amongst drugs, there is a pressing need for new and potent IN inhibitors. This review covers the three patents describing spirocyclic and phosphate substituted quinolizine derivatives as novel HIV-1 IN inhibitors for the discovery of new anti-HIV-1 drug candidates. Areas covered: This review is focused on spirocyclic and phosphate substituted quinolizine derivatives bearing the same metal chelation scaffold as novel HIV-1 IN inhibitors. Expert Opinion: Generally, privileged structure-based optimizations have emerged as an effective approach to discover newly antiviral agents. More generally, due to the similar Mg(2+) catalytic active centers of endoribonucleases, some divalent metal ion chelators were found to be versatile binders targeting multiple metalloenzymes. Therefore, privileged structure-based scaffold re-evolution is an important tactic to identify new chemotypes, to explore unknown biological activities, or to provide effective ligands for multiple targets by modifying the existing active compounds.

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