Design, Synthesis, and Biological Evaluation of Highly Potent Small Molecule–Peptide Conjugates as New HIV-1 Fusion Inhibitors

2013 ◽  
Vol 56 (6) ◽  
pp. 2527-2539 ◽  
Author(s):  
Chao Wang ◽  
Weiguo Shi ◽  
Lifeng Cai ◽  
Lu Lu ◽  
Qian Wang ◽  
...  
Keyword(s):  
Small Molecule ◽  
Biological Evaluation ◽  
Peptide Conjugates ◽  
Design Synthesis ◽  
Fusion Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

Design, synthesis and biological evaluation of novel 5-((substituted quinolin-3-yl/1-naphthyl) methylene)-3-substituted imidazolidin-2,4-dione as HIV-1 fusion inhibitors

2020 ◽  
Vol 99 ◽  
pp. 103782 ◽  
Author(s):  
Tarek S. Ibrahim ◽  
Riham M. Bokhtia ◽  
Amany M.M. AL-Mahmoudy ◽  
Ehab S. Taher ◽  
Mohammed A. AlAwadh ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Fusion Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

The Discovery and Development of Oxalamide and Pyrrole Small Molecule Inhibitors of gp120 and HIV Entry - A Review

2019 ◽  
Vol 19 (18) ◽  
pp. 1650-1675 ◽  
Author(s):  
Damoder Reddy Motati ◽  
Dilipkumar Uredi ◽  
E. Blake Watkins
Keyword(s):  
Small Molecule ◽  
Viral Entry ◽  
Biological Evaluation ◽  
New Drugs ◽  
Design Synthesis ◽  
Mortality And Morbidity ◽  
Glycoprotein Gp120 ◽  
Hiv Entry ◽  
Immunodeficiency Syndrome ◽  
Hiv 1

Human immunodeficiency virus type-1 (HIV-1) is the causative agent responsible for the acquired immunodeficiency syndrome (AIDS) pandemic. More than 60 million infections and 25 million deaths have occurred since AIDS was first identified in the early 1980s. Advances in available therapeutics, in particular combination antiretroviral therapy, have significantly improved the treatment of HIV infection and have facilitated the shift from high mortality and morbidity to that of a manageable chronic disease. Unfortunately, none of the currently available drugs are curative of HIV. To deal with the rapid emergence of drug resistance, off-target effects, and the overall difficulty of eradicating the virus, an urgent need exists to develop new drugs, especially against targets critically important for the HIV-1 life cycle. Viral entry, which involves the interaction of the surface envelope glycoprotein, gp120, with the cellular receptor, CD4, is the first step of HIV-1 infection. Gp120 has been validated as an attractive target for anti-HIV-1 drug design or novel HIV detection tools. Several small molecule gp120 antagonists are currently under investigation as potential entry inhibitors. Pyrrole, piperazine, triazole, pyrazolinone, oxalamide, and piperidine derivatives, among others, have been investigated as gp120 antagonist candidates. Herein, we discuss the current state of research with respect to the design, synthesis and biological evaluation of oxalamide derivatives and five-membered heterocycles, namely, the pyrrole-containing small molecule as inhibitors of gp120 and HIV entry.

Design, synthesis and biological evaluation of imidazole and oxazole fragments as HIV-1 integrase-LEDGF/p75 disruptors and inhibitors of microbial pathogens

2020 ◽  
Vol 28 (1) ◽  
pp. 115210 ◽  
Author(s):  
Thompho J. Rashamuse ◽  
Angela T. Harrison ◽  
Salerwe Mosebi ◽  
Sandy van Vuuren ◽  
E. Mabel Coyanis ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Microbial Pathogens ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1
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