Design and synthesis of novel pyrimidone analogues as HIV-1 integrase inhibitors

2^nd International Conference on Medicinal Chemistry & Computer Aided Drug Designing

October 15-17, 2013 Hampton Inn Tropicana, Las Vegas, NV, USA

Guisen Zhao, Shenghui Yu, Tino Wilson Sanchez and Nouri Neamati

Scientific Tracks Abstracts: Med chem

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. Keywords: HIV-1, Integrase inhibitors, Pyrimidone analogues.