Abstract：
:Influenza virus (IFV) causes periodic global influenza pandemics, resulting in substantial socioeconomic loss and burden on medical facilities. Yearly variation in the effectiveness of vaccines, slow responsiveness to vaccination in cases of pandemic IFV, and emerging resistance to available drugs highlight the need to develop additional small-molecular inhibitors that act on IFV proteins. One promising target is polymerase acidic (PA) endonuclease, which is a bridged dinuclear metalloenzyme that plays a crucial role in initiating IFV replication. During the past decade, intensive efforts have been made to develop small-molecular inhibitors of this endonuclease as candidate agents for treatment of IFV infection. Here, we review the current status of development of PA endonuclease inhibitors and we discuss the applicability of newer medicinal-chemistry strategies for the discovery more potent, selective, and safer inhibitors.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Ju H,Zhang J,Huang B,Kang D,Huang B,Liu X,Zhan Pdoi
10.1021/acs.jmedchem.6b01227subject
Has Abstractpub_date
2017-05-11 00:00:00pages
3533-3551issue
9eissn
0022-2623issn
1520-4804journal_volume
60pub_type
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