Design, synthesis and antiviral activity of novel quinazolinones

Z Wang, M Wang, X Yao, Y Li, J Tan, L Wang… - European journal of …, 2012 - Elsevier
HIV-1 integrase (IN) is a validated therapeutic target for antiviral drug design. However, the
emergence of viral strains resistant to clinically studied IN inhibitors demands the discovery …

Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity

C Bénard, F Zouhiri, M Normand-Bayle, M Danet… - Bioorganic & medicinal …, 2004 - Elsevier
A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and
ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an …

Design and Synthesis of Novel N-Hydroxy-Dihydronaphthyridinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors

TW Johnson, SP Tanis, SL Butler… - Journal of medicinal …, 2011 - ACS Publications
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential
for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of …

4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors

M Billamboz, V Suchaud, F Bailly, C Lion… - ACS Medicinal …, 2013 - ACS Publications
A series of 2-hydroxy-1, 3-dioxoisoquinoline-4-carboxamides featuring an N-hydroxyimide
chelating functionality was evaluated for their inhibitory properties against human …

De novo design and synthesis of HIV-1 integrase inhibitors

MT Makhija, RT Kasliwal, VM Kulkarni… - Bioorganic & medicinal …, 2004 - Elsevier
Existing AIDS therapies are out of reach for most HIV-infected people in developing
countries and, where available, they are limited by their toxicity and their cost. New anti-HIV …

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors

E Muraglia, O Kinzel, C Gardelli… - Journal of medicinal …, 2008 - ACS Publications
HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral
replication, but integrase inhibitors as marketed drugs have just very recently started to …

Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors

MB Plewe, SL Butler, K R. Dress, Q Hu… - Journal of medicinal …, 2009 - ACS Publications
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential
for viral replication. Recently, HIV-1 IN inhibitors have emerged as a new promising class of …

Design, synthesis, and biological evaluation of 1, 2-dihydroisoquinolines as HIV-1 integrase inhibitors

V Tandon, Urvashi, P Yadav, S Sur… - ACS Medicinal …, 2015 - ACS Publications
6-Endo-dig-cyclization is an efficient method for the synthesis of 1, 2-dihydroisoquinolines.
We have synthesized few 1, 2-dihydroisoquinolines having different functionality at the C-1 …

Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring

SE Metobo, H Jin, M Tsiang, CU Kim - Bioorganic & medicinal chemistry …, 2006 - Elsevier
This communication details both the syntheses and biological evaluation of a novel class of
HIV-1 integrase inhibitors. When the quinoline moiety is replaced with the quinoxoline …

Quinoline-based HIV integrase inhibitors

R Musiol - Current pharmaceutical design, 2013 - ingentaconnect.com
HIV integrase became an important target for drug development more than twenty years
ago. However, progress has been hampered by the lack of assays suitable for high …