Abstract:
:A series of novel pyrimidone analogues have been designed and synthesized as HIV-1 integrase (IN) inhibitors. This study demonstrated that introducing a substituent in the N1-position of the pyrimidone scaffold does not significantly influence IN inhibitory activity. Molecular docking studies showed these compounds could occupy the IN active site and form pi-pi interactions with viral DNA nucleotides DC16 and DA17 to displace reactive viral DNA 3'OH and block intasome activity.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Yu S,Sanchez TW,Liu Y,Yin Y,Neamati N,Zhao Gdoi
10.1016/j.bmcl.2013.09.018subject
Has Abstractpub_date
2013-11-15 00:00:00pages
6134-7issue
22eissn
0960-894Xissn
1464-3405pii
S0960-894X(13)01081-0journal_volume
23pub_type
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