Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives

2016 ◽  
Vol 67 ◽  
pp. 75-83 ◽  
Author(s):  
Subhash Chander ◽  
Ping Wang ◽  
Penta Ashok ◽  
Liu-Meng Yang ◽  
Yong-Tang Zheng ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Rational Design ◽  
Design Synthesis ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation

2020 ◽  
Vol 63 (4) ◽  
pp. 1724-1749
Author(s):  
Francesca Curreli ◽  
Shahad Ahmed ◽  
Sofia M. Benedict Victor ◽  
Ildar R. Iusupov ◽  
Dmitry S. Belov ◽  
...  
Keyword(s):  
Rational Design ◽  
Design Synthesis ◽  
Adme Properties ◽  
Anti Hiv ◽  
Hiv 1

Rational Design, Synthesis, Anti-HIV-1 RT and Anti-microbial Activity of Novel 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-phenylpropanamide Derivatives

2016 ◽  
Vol 14 (1) ◽  
pp. 63-73
Author(s):  
Subhash Chander ◽  
Penta Ashok ◽  
Rajnish P. Singh ◽  
Prabhat N. Jha ◽  
Yong-Tang Zheng ◽  
...  
Keyword(s):  
Microbial Activity ◽  
Rational Design ◽  
Design Synthesis ◽  
Anti Hiv ◽  
Hiv 1

Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors

2016 ◽  
Vol 24 (9) ◽  
pp. 2125-2136 ◽  
Author(s):  
Liang Yang ◽  
Ping Wang ◽  
Ji-Feng Wu ◽  
Liu-Meng Yang ◽  
Rui-Rui Wang ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals Design, Synthesis and Docking Studies of Novel 1, 2, 3-Triazolyl Phenylthiazole Analogs as Potent Anti-HIV-1 NNRT Inhibitors

2017 ◽  
Vol 7 (10) ◽  
Author(s):  
Suresh C Jadhavar ◽  
Sujit G Bhansali ◽  
Shivaji B Patwari ◽  
Sudhakar R Bhusare ◽  
Hanmant M Kasralikar
Keyword(s):  
Docking Studies ◽  
Design Synthesis ◽  
Anti Hiv ◽  
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.

scholarly journals Design, Synthesis and Docking Studies of New 4-hydroxyquinoline-3-carbohydrazide Derivatives as Anti-HIV-1 Agents

Drug Research ◽  
2013 ◽  
Vol 63 (04) ◽  
pp. 192-197 ◽  
Author(s):  
Z. Hajimahdi ◽  
R. Zabihollahi ◽  
M. Aghasadeghi ◽  
A. Zarghi
Keyword(s):  
Docking Studies ◽  
Design Synthesis ◽  
Anti Hiv ◽  
Hiv 1

Anti HIV-1 and antimicrobial activity of the leaf extracts of Calotropis procera

2010 ◽  
Vol 4 (4) ◽  
pp. 242 ◽  
Author(s):  
Remya Mohanraj ◽  
Jyotirmoy Rakshit ◽  
Malcolm Nobre
Keyword(s):  
Antimicrobial Activity ◽  
Calotropis Procera ◽  
Leaf Extracts ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals Design, synthesis, and anti-HIV-1 activity of 1-aromatic methyl-substituted 3-(3,5-dimethylbenzyl)uracil and N-3,5-dimethylbenzyl-substituted urea derivatives

2015 ◽  
Vol 24 (1) ◽  
pp. 3-18 ◽  
Author(s):  
Norikazu Sakakibara ◽  
Masanori Baba ◽  
Mika Okamoto ◽  
Masaaki Toyama ◽  
Yosuke Demizu ◽  
...  
Keyword(s):  
Urea Derivatives ◽  
Design Synthesis ◽  
Anti Hiv ◽  
Hiv 1 ◽  
Substituted Urea

scholarly journals Design, synthesis, and anti-HIV-1 activity of 1-substituted 3-(3,5-dimethylbenzyl)triazine derivatives

2015 ◽  
Vol 24 (2) ◽  
pp. 62-71 ◽  
Author(s):  
Norikazu Sakakibara ◽  
Gianfranco Balboni ◽  
Cenzo Congiu ◽  
Valentina Onnis ◽  
Yosuke Demizu ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Triazine Derivatives ◽  
Anti Hiv ◽  
Hiv 1

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs

2017 ◽  
Vol 140 ◽  
pp. 383-391 ◽  
Author(s):  
Zhaoqiang Liu ◽  
Ye Tian ◽  
Jinghan Liu ◽  
Boshi Huang ◽  
Dongwei Kang ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Anti Hiv ◽  
Hiv 1
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