scholarly journals Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors

Molecules ◽  
2008 ◽  
Vol 13 (10) ◽  
pp. 2442-2461 ◽  
Author(s):  
Mario Sechi ◽  
Ugo Azzena ◽  
Maria Paola Delussu ◽  
Roberto Dallocchio ◽  
Alessandro Dessì ◽  
...  
Keyword(s):  
Malonic Acid ◽  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Derivatives Of ◽  
Hiv 1

scholarly journals The design and synthesis of a pyrrole-carbaldehyde hit family as HIV-1 integrase inhibitors

2011 ◽  
Vol 30 (1) ◽  
Author(s):  
Telisha Traut ◽  
Raymond Hewer ◽  
Judy Coates ◽  
D. Bradley G. Williams
Keyword(s):  
Water Soluble ◽  
Integrase Inhibitors ◽  
Compound Library ◽  
One Pot ◽  
Design And Synthesis ◽  
Chemical Structures ◽  
In Silico Predictions ◽  
Further Development ◽  
Derivatives Of ◽  
Hiv 1

Screening of an HIV-1 IN model against database-derived chemical structures identified pyrrole-carbaldehydes as targets for further development. Chemical synthesis using a facile one-pot reaction resulted in the generation of a compound library. Preliminary toxicity and efficacy assays of the water-soluble HCl-salt derivatives of each compound support the in silico predictions.

scholarly journals Structural-Functional Analysis of 2,1,3-Benzoxadiazoles and Their N-oxides As HIV-1 Integrase Inhibitors

Acta Naturae ◽  
2013 ◽  
Vol 5 (1) ◽  
pp. 63-72 ◽  
Author(s):  
S. P. Korolev ◽  
O. V. Kondrashina ◽  
D. S. Druzhilovsky ◽  
A. M. Starosotnikov ◽  
M. D. Dutov ◽  
...  
Keyword(s):  
Integrase Inhibitor ◽  
Integrase Inhibitors ◽  
Mechanism Of Inhibition ◽  
Immunodeficiency Virus ◽  
Pharmacokinetic Properties ◽  
Nitro Derivatives ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

Human immunodeficiency virus type 1 integrase is one of the most attractive targets for the development of anti-HIV-1 inhibitors. The capacity of a series of 2,1,3-benzoxadiazoles (benzofurazans) and their N-oxides (benzofuroxans) selected using the PASS software to inhibit the catalytic activity of HIV-1 integrase was studied in the present work. Only the nitro-derivatives of these compounds were found to display inhibitory activity. The study of the mechanism of inhibition by nitro-benzofurazans/benzofuroxans showed that they impede the substrate DNA binding at the integrase active site. These inhibitors were also active against integrase mutants resistant to raltegravir, which is the first HIV-1 integrase inhibitor approved for clinical use. The comparison of computer-aided estimations of the pharmacodynamic and pharmacokinetic properties of the compounds studied and raltegravir led us to conclude that these compounds show promise and need to be further studied as potential HIV-1 integrase inhibitors.

scholarly journals Design and Synthesis of Novel Indole β-Diketo Acid Derivatives as HIV-1 Integrase Inhibitors

2004 ◽  
Vol 47 (21) ◽  
pp. 5298-5310 ◽  
Author(s):  
Mario Sechi ◽  
Massimiliano Derudas ◽  
Roberto Dallocchio ◽  
Alessandro Dessì ◽  
Alessia Bacchi ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Hiv 1

Design and Synthesis of Photoactivatable Aryl Diketo Acid-Containing HIV-1 Integrase Inhibitors (I) as Potential Affinity Probes.

ChemInform ◽  
2004 ◽  
Vol 35 (23) ◽  
Author(s):  
Xuechun Zhang ◽  
Christophe Marchand ◽  
Yves Pommier ◽  
Terrence R. Jr. Burke
Keyword(s):  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Affinity Probes ◽  
Hiv 1

Design and Synthesis of Bicyclic Pyrimidinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors

2008 ◽  
Vol 51 (4) ◽  
pp. 861-874 ◽  
Author(s):  
Ester Muraglia ◽  
Olaf Kinzel ◽  
Cristina Gardelli ◽  
Benedetta Crescenzi ◽  
Monica Donghi ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Orally Bioavailable ◽  
Hiv 1

De novo design and synthesis of HIV-1 integrase inhibitors

2004 ◽  
Vol 12 (9) ◽  
pp. 2317-2333 ◽  
Author(s):  
Mahindra T Makhija ◽  
Rajesh T Kasliwal ◽  
Vithal M Kulkarni ◽  
Nouri Neamati
Keyword(s):  
De Novo ◽  
De Novo Design ◽  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Hiv 1

Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors

2009 ◽  
Vol 17 (7) ◽  
pp. 2925-2935 ◽  
Author(s):  
Mario Sechi ◽  
Giuseppe Rizzi ◽  
Alessia Bacchi ◽  
Mauro Carcelli ◽  
Dominga Rogolino ◽  
...  
Keyword(s):  
Carboxylic Acids ◽  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Hiv 1

Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors

2008 ◽  
Vol 18 (2) ◽  
pp. 721-725 ◽  
Author(s):  
H. Marie Langford ◽  
Peter D. Williams ◽  
Carl F. Homnick ◽  
Joseph P. Vacca ◽  
Peter J. Felock ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Hiv 1

Design and synthesis of N-methylpyrimidone derivatives as HIV-1 integrase inhibitors

2015 ◽  
Vol 23 (4) ◽  
pp. 735-741 ◽  
Author(s):  
Yujie Wang ◽  
Jie Rong ◽  
Bin Zhang ◽  
Liming Hu ◽  
Xiaoli Wang ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Hiv 1

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

2013 ◽  
Vol 23 (22) ◽  
pp. 6134-6137 ◽  
Author(s):  
Shenghui Yu ◽  
Tino Wilson Sanchez ◽  
Yang Liu ◽  
Yanzhen Yin ◽  
Nouri Neamati ◽  
...  
Keyword(s):  
Integrase Inhibitors ◽  
Design And Synthesis ◽  
Hiv 1
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