Design, Synthesis, Screening, and Decoding of Encoded One-bead One-compound Peptidomimetic and Small Molecule Combinatorial Libraries

ChemInform ◽  
2005 ◽  
Vol 36 (4) ◽  
Author(s):  
Ruiwu Liu ◽  
Jan Marik ◽  
Kit S. Lam
Keyword(s):  
Small Molecule ◽  
Combinatorial Libraries ◽  
Design Synthesis

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 Evaluation of Quinoline-based Small Molecule Inhibitor of STAT3

2013 ◽  
Vol 10 (5) ◽  
pp. 420-426 ◽  
Author(s):  
Zhi-Bing Shi ◽  
Lei Zhang ◽  
Zheng-Yang Bin ◽  
Xiang-Rong Cao ◽  
Zhu-Nan Gong ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Design Synthesis ◽  
Molecule Inhibitor

scholarly journals Design, Synthesis, and antiviral activity of a series of CD4-mimetic small-molecule HIV-1 entry inhibitors

2021 ◽  
pp. 116000
Author(s):  
Francesca Curreli ◽  
Shahad Ahmed ◽  
Sofia M. Benedict Victor ◽  
Ildar R. Iusupov ◽  
Evgeny A. Spiridonov ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Small Molecule ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Hiv 1

scholarly journals Enabling Large-Scale Design, Synthesis and Validation of Small Molecule Protein-Protein Antagonists

PLoS ONE ◽  
2012 ◽  
Vol 7 (3) ◽  
pp. e32839 ◽  
Author(s):  
David Koes ◽  
Kareem Khoury ◽  
Yijun Huang ◽  
Wei Wang ◽  
Michal Bista ◽  
...  
Keyword(s):  
Small Molecule ◽  
Large Scale ◽  
Design Synthesis ◽  
Scale Design

Lipoic acid based core cross-linked micelles for multivalent platforms: design, synthesis and application in bio-imaging and drug delivery

2017 ◽  
Vol 15 (22) ◽  
pp. 4798-4802 ◽  
Author(s):  
Jingsheng Huang ◽  
Fang Wu ◽  
Yunlong Yu ◽  
Haolong Huang ◽  
Shiyong Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Small Molecule ◽  
Lipoic Acid ◽  
Design Synthesis ◽  
Bio Imaging

Natural lipoic acid derived small-molecule amphiphiles self-assemble into micelles in water.

Sign in / Sign up

Export Citation Format

Share Document