Synthesis and anti-HIV activity of GS-9148 (2′-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor

2008 ◽  
Vol 18 (3) ◽  
pp. 1120-1123 ◽  
Author(s):  
Constantine G. Boojamra ◽  
Richard L. Mackman ◽  
David Y. Markevitch ◽  
Vidya Prasad ◽  
Adrian S. Ray ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitor ◽  
Anti Hiv

ChemInform Abstract: Synthesis and anti-HIV Activity of GS-9148 (2′-Fd4AP), a Novel Nucleoside Phosphonate HIV Reverse Transcriptase Inhibitor.

ChemInform ◽  
2008 ◽  
Vol 39 (28) ◽  
Author(s):  
Constantine G. Boojamra ◽  
Richard L. Mackman ◽  
David Y. Markevitch ◽  
Vidya Prasad ◽  
Adrian S. Ray ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitor ◽  
Anti Hiv

Structure and conformational analysis of the anti-HIV reverse transcriptase inhibitor AZT using MP2 and DFT methods. Differences with the natural nucleoside thymidine. Simulation of the 1st phosphorylation step with ATP

2014 ◽  
Vol 16 (45) ◽  
pp. 24763-24783 ◽  
Author(s):  
M. Alcolea Palafox
Keyword(s):  
Proton Transfer ◽  
Conformational Analysis ◽  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Transfer Mechanism ◽  
Hiv Reverse Transcriptase ◽  
Dft Methods ◽  
Reverse Transcriptase Inhibitor ◽  
Anti Hiv ◽  
Hiv 1

A proton-transfer mechanism is proposed for the first phosphorylation step of the nucleoside HIV-1 reverse transcriptase inhibitor AZT (3′-azido-3′ deoxythymidine) by interacting with ATP.

Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor

2016 ◽  
Vol 59 (5) ◽  
pp. 1891-1898 ◽  
Author(s):  
Cyril Dousson ◽  
François-René Alexandre ◽  
Agnès Amador ◽  
Séverine Bonaric ◽  
Stéphanie Bot ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Nucleoside Reverse Transcriptase Inhibitor ◽  
Transcriptase Inhibitor ◽  
Reverse Transcriptase Inhibitor ◽  
Anti Hiv

Enzymatic kinetic studies with the non-nucleoside HIV reverse transcriptase inhibitor U-9843

1992 ◽  
Vol 48 (11-12) ◽  
pp. 1127-1132 ◽  
Author(s):  
I. W. Althaus ◽  
R. J. LeMay ◽  
A. J. Gonzales ◽  
M. R. Deibel ◽  
S. K. Sharma ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Kinetic Studies ◽  
Transcriptase Inhibitor ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitor

Synthesis and oxidation of 2-hydroxynevirapine, a metabolite of the HIV reverse transcriptase inhibitor nevirapine

2011 ◽  
Vol 9 (22) ◽  
pp. 7822 ◽  
Author(s):  
Alexandra M. M. Antunes ◽  
David A. Novais ◽  
J. L. Ferreira da Silva ◽  
Pedro P. Santos ◽  
M. Conceição Oliveira ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitor

scholarly journals Synthesis of 1-benzyl-3-(3,5-dimethylbenzyl)Uracil Derivatives with Potential Anti-HIV Activity

2011 ◽  
Vol 22 (2) ◽  
pp. 57-65 ◽  
Author(s):  
Yohei Isono ◽  
Norikazu Sakakibara ◽  
Paula Ordonez ◽  
Takayuki Hamasaki ◽  
Masanori Baba ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Structural Modifications ◽  
Half Maximal Effective Concentration ◽  
Reverse Transcriptase Inhibitor ◽  
Anti Hiv Agents ◽  
Substituted 1 ◽  
Anti Hiv ◽  
Hiv 1

Background: Nine novel uracil analogues were synthesized and evaluated as inhibitors of HIV-1. Methods: Key structural modifications included replacement of the 6-chloro group of 1-benzyl-6-chloro-3-(3,5-dimethylbenzyl)uracil by other functional groups or N1-alkylation of 3-(3,5-dimethylbenzyl)-5-fluorouracil. Results: These compounds showed only micromolar potency against HIV-1 in MT-4, though two of them; 6-azido-1-benzyl-3-(3,5-dimethylbenzyl) uracil and 6-amino-1-benzyl-3-(3,5-dimethylbenzyl) uracil were highly potent (half maximal effective concentration =0.067 and 0.069 μM) and selective (selectivity index =685 and 661), respectively. Structure–activity relationships among the newly synthesized uracil analogues suggest the importance of the H-bond formed between 6-amino group of 6-amino-1-benzyl-3-(3,5-dimethylbenzyl) uracil and amide group of HIV-1 reverse transcriptase. Conclusions: We discovered two 6-substituted 1-benzyl-3-(3,5-dimethylbenzyl) uracils, (6-azido-1-benzyl-3-(3,5-dimethylbenzyl) uracil and 6-amino-1-benzyl-3-(3,5-dimethylbenzyl) uracil) as novel anti-HIV agents. These compounds should be further pursued for their toxicity and pharmacokinetics in vivo as well as antiviral activity against non-nucleoside reverse transcriptase inhibitor-resistant strains.

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