HIV-1 Resistance to Integrase Inhibitors

2017 ◽  
pp. 559-564
Author(s):  
Ying-Shan Han ◽  
Thibault Mesplède ◽  
Mark A. Wainberg
Keyword(s):  
Integrase Inhibitors ◽  
Hiv 1

Design, Synthesis and Biological Activity of Aromatic Diketone Derivatives as HIV-1 Integrase Inhibitors

2015 ◽  
Vol 11 (2) ◽  
pp. 180-187 ◽  
Author(s):  
Liming Hu ◽  
Zhipeng Li ◽  
Zhanyang Wang ◽  
Gengxin Liu ◽  
Xianzhuo He ◽  
...  
Keyword(s):  
Biological Activity ◽  
Integrase Inhibitors ◽  
Design Synthesis ◽  
Hiv 1

scholarly journals HIV-1 resistance patterns to integrase inhibitors in Chilean patients with virological failure on raltegravir-containing regimens

2020 ◽  
Vol 6 (3) ◽  
pp. 100002
Author(s):  
Pablo Ferrer ◽  
Consuelo Rodriguez ◽  
Alicia Sciaraffia ◽  
Rocío Tordecilla ◽  
Veronica Ramos ◽  
...  
Keyword(s):  
Virological Failure ◽  
Integrase Inhibitors ◽  
Resistance Patterns ◽  
Hiv 1

New 4-[(1-Benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, β-Diketo Acid Analogues as HIV-1 Integrase Inhibitors.

ChemInform ◽  
2007 ◽  
Vol 38 (41) ◽  
Author(s):  
Stefania Ferro ◽  
Maria Letizia Barreca ◽  
Laura De Luca ◽  
Angela Rao ◽  
Anna Maria Monforte ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Hiv 1

Novel furocoumarins as potential HIV-1 integrase inhibitors

2014 ◽  
Vol 57 ◽  
pp. 1-4 ◽  
Author(s):  
Temitope O. Olomola ◽  
Salerwe Mosebi ◽  
Rosalyn Klein ◽  
Telisha Traut-Johnstone ◽  
Judy Coates ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Hiv 1

Novel HIV-1 Integrase Inhibitors Derived from Quinolone Antibiotics

2006 ◽  
Vol 49 (5) ◽  
pp. 1506-1508 ◽  
Author(s):  
Motohide Sato ◽  
Takahisa Motomura ◽  
Hisateru Aramaki ◽  
Takashi Matsuda ◽  
Masaki Yamashita ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Quinolone Antibiotics ◽  
Hiv 1

3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates—A new class of HIV-1 integrase inhibitors

2009 ◽  
Vol 19 (7) ◽  
pp. 1930-1934 ◽  
Author(s):  
Monica Donghi ◽  
Olaf D. Kinzel ◽  
Vincenzo Summa
Keyword(s):  
Integrase Inhibitors ◽  
New Class ◽  
Hiv 1

Mining the NCI antiviral compounds for HIV-1 integrase inhibitors

2006 ◽  
Vol 14 (11) ◽  
pp. 3785-3792 ◽  
Author(s):  
Jinxia Deng ◽  
James A. Kelley ◽  
Joseph J. Barchi ◽  
Tino Sanchez ◽  
Raveendra Dayam ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Antiviral Compounds ◽  
Hiv 1

Design, Synthesis and Docking Studies of Thioimidazolyl Diketoacid Derivatives Targeting HIV-1 Integrase

2021 ◽  
Vol 17 ◽  
Author(s):  
Nafiseh Karimi ◽  
Rouhollah Vahabpour Roudsari ◽  
Zahra Hajimahdi ◽  
Afshin Zarghi
Keyword(s):  
Drug Target ◽  
Enzyme Assay ◽  
Binding Mode ◽  
Docking Studies ◽  
Integrase Inhibitors ◽  
Design Synthesis ◽  
Ic50 Values ◽  
Novel Structures ◽  
Anti Hiv ◽  
Hiv 1

Background: Integrase enzyme is a validated drug target to discover novel structures as anti-HIV-1 agents. Objective: Novel series of thioimidazolyl diketo acid derivatives characterizing various substituents at N-1 and 2-thio positions of central ring were developed as HIV-1 integrase inhibitors. Results: The obtained molecules were evaluated in the enzyme assay, displaying promising integrase inhibitory activity with IC50 values ranging from 0.9 to 7.7 M. The synthesized compounds were also tested for antiviral activity and cytotoxicity using HeLa cells infected by the single-cycle replicable HIV-1 NL4-3. Conclusion: The most potent compound was 18i with EC50=19 µM, IC50 0.9 µM and SI= 10.5. Docking studies indicated that the binding mode of the active molecule is well aligned with the known HIV-1 integrase inhibitors.

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