Synthesis, SAR, and Biological Evaluation of Oximino-Piperidino-Piperidine Amides. 1. Orally Bioavailable CCR5 Receptor Antagonists with Potent Anti-HIV Activity

2002 ◽  
Vol 45 (14) ◽  
pp. 3143-3160 ◽  
Author(s):  
Anandan Palani ◽  
Sherry Shapiro ◽  
Hubert Josien ◽  
Thomas Bara ◽  
John W. Clader ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Receptor Antagonists ◽  
Ccr5 Receptor ◽  
Orally Bioavailable ◽  
Anti Hiv

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity

2002 ◽  
Vol 12 (20) ◽  
pp. 2997-3000 ◽  
Author(s):  
Jeffrey J Hale ◽  
Richard J Budhu ◽  
Sander G Mills ◽  
Malcolm MacCoss ◽  
Sandra L Gould ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Ccr5 Receptor ◽  
Anti Hiv ◽  
Hiv 1

Synthetic Strategies, Chemical Reactivities and Biological Activities of 3-Thioxo-1,2,4-Triazin-5-Ones and Their Derivatives

2019 ◽  
Vol 16 (4) ◽  
pp. 308-322
Author(s):  
Mohammad S.T. Makki ◽  
Reda M. Abdel-Rahman ◽  
Abdulrahman S. Alharbi
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Literature Survey ◽  
Recent Advances ◽  
Nucleophilic Reagents ◽  
Anti Hiv ◽  
Biological Field

In recent years, a very interest in the synthesis of functionalized 3-thioxo-1,2,4-triazin-5- ones and their derivatives as vital probes has been increased, due to the important, applications of the medicinal, pharmacological, and biological field as a drug, semi drug, and bioactive systems. The present work review outlines extensive recent advances literature survey on the synthesis of sulfurbearing 1,2,4-triazin-5-one derivatives has been reconsidered. Also, the behavior of these family towards electrophilic and nucleophilic reagents in different media and conditions reported. The biological evaluation of the most synthesized systems included anticancer, anti-HIV, antimicrobial as well as their enzymatic effects (cellobiase produced by fungi) have been reported. The reactivity of these systems depends on the polarity of solvent, temperature, molarity as well as a type of tautomeric present.

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