4-Benzyl- and 4-Benzoyl-3-dimethylaminopyridin-2(1H)-ones, a New Family of Potent Anti-HIV Agents:  Optimization and in Vitro Evaluation against Clinically Important HIV Mutant Strains

2004 ◽  
Vol 47 (22) ◽  
pp. 5501-5514 ◽  
Author(s):  
Abdellah Benjahad ◽  
Karine Courté ◽  
Jérôme Guillemont ◽  
Dominique Mabire ◽  
Sophie Coupa ◽  
...  
Keyword(s):  
In Vitro Evaluation ◽  
New Family ◽  
Mutant Strains ◽  
Anti Hiv Agents ◽  
Anti Hiv

In vitro evaluation of phosphocholine and quaternary ammonium containing lipids as novel anti-HIV agents

1991 ◽  
Vol 34 (4) ◽  
pp. 1377-1383 ◽  
Author(s):  
Karen L. Meyer ◽  
Canino J. Marasco ◽  
Susan L. Morris-Natschke ◽  
Khalid S. Ishaq ◽  
Claude Piantadosi ◽  
...  
Keyword(s):  
Quaternary Ammonium ◽  
In Vitro Evaluation ◽  
Anti Hiv Agents ◽  
Anti Hiv

scholarly journals A Novel Class of Anti-HIV Agents with Multiple Copies of Enfuvirtide Enhances Inhibition of Viral Replication and Cellular Transmission In Vitro

PLoS ONE ◽  
2012 ◽  
Vol 7 (7) ◽  
pp. e41235 ◽  
Author(s):  
Chien-Hsing Chang ◽  
Jorma Hinkula ◽  
Meiyu Loo ◽  
Tina Falkeborn ◽  
Rongxiu Li ◽  
...  
Keyword(s):  
Viral Replication ◽  
Multiple Copies ◽  
Anti Hiv Agents ◽  
Anti Hiv

In vitro evaluation of leishmanicidal properties of a new family of monodimensional coordination polymers based on diclofenac ligand

Polyhedron ◽  
2020 ◽  
Vol 184 ◽  
pp. 114570 ◽  
Author(s):  
Amalia García-García ◽  
José M. Méndez-Arriaga ◽  
Rubén Martín-Escolano ◽  
Javier Cepeda ◽  
Santiago Gómez-Ruiz ◽  
...  
Keyword(s):  
Coordination Polymers ◽  
In Vitro Evaluation ◽  
New Family

Phenyl phosphoramidate derivatives of stavudine as anti-HIV agents with potent and selective in-vitro antiviral activity against Adenovirus

2004 ◽  
Vol 39 (3) ◽  
pp. 225-234 ◽  
Author(s):  
Fatih M. Uckun ◽  
Sharon Pendergrass ◽  
Sanjive Qazi ◽  
P. Samuel ◽  
T.K. Venkatachalam
Keyword(s):  
Antiviral Activity ◽  
Anti Hiv Agents ◽  
Derivatives Of ◽  
Anti Hiv

scholarly journals Synthesis and Evaluation of Some Symmetrical Phosphate Dimer Derivatives of 3′-Modified Nucleosides as Potential anti-HIV Agents

1996 ◽  
Vol 7 (6) ◽  
pp. 330-337 ◽  
Author(s):  
C. McGuigan ◽  
H.-W. Tsang ◽  
N. Mahmood ◽  
A. J. Hay
Keyword(s):  
Human Immunodeficiency Virus ◽  
Analytical Data ◽  
Modified Nucleosides ◽  
Nucleoside Analogues ◽  
Immunodeficiency Virus ◽  
Anti Hiv Agents ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

Novel symmetrical nucIeotide-(5′,5′)-dimers of 3′-O-acetylthymidine, 3′-O-methylthymidine, 3′-O-ethylthymidine, 3′-O-n-propylthymidine and 3′-azido-3′-deoxythymidine (AZT) were synthesized as membrane soluble pro-drugs. These were prepared using phosphorodichloridate chemistry and were characterised by spectroscopic and analytical data. In-vitro evaluation of the derivatives in cells acutely infected with the human immunodeficiency virus (HIV-1) demonstrated a range of activities. These derivatives were generally found to display poor inhibition of HIV proliferation. Derivatives containing AZT moieties were found to be potent, but such compounds were less active than the parent nucleoside. The data indicated that the AZT-containing compounds act primarily via the release of the free nucleoside. However, in some cases, the dimers of certain inactive nucleoside analogues were found to be active. In these cases, release of the nucleoside alone cannot account for the activity.

ChemInform Abstract: Anti-HIV Agents. Part 1. Synthesis and in vitro Anti-HIV Evaluation of Novel in 1H,3H-Thiazolo(3,4-a)benzimidazoles.

ChemInform ◽  
2010 ◽  
Vol 23 (20) ◽  
pp. no-no
Author(s):  
A. CHIMIRRI ◽  
S. GRASSO ◽  
A.-M. MONFORTE ◽  
P. MONFORTE ◽  
M. ZAPPALA
Keyword(s):  
Anti Hiv Agents ◽  
Anti Hiv

In Vitro Evaluation of Leishmanicidal Properties of a New Family of Monodimensional Coordination Polymers Based on Diclofenac Ligand

2020 ◽  
Author(s):  
Amalia García-García ◽  
José Manuel Méndez ◽  
Rubén Martín-Escolano ◽  
Javier Cepeda ◽  
Santiago Gómez-Ruiz ◽  
...  
Keyword(s):  
Coordination Polymers ◽  
In Vitro Evaluation ◽  
New Family

Phenyl Phosphoramidate Derivatives of Stavudine as anti-HIV Agents with Potent and Selective in-vitro Antiviral Activity Against Adenovirus.

ChemInform ◽  
2004 ◽  
Vol 35 (35) ◽  
Author(s):  
Fatih M. Uckun ◽  
Sharon Pendergrass ◽  
Sanjive Qazi ◽  
P. Samuel ◽  
T. K. Venkatachalam
Keyword(s):  
Antiviral Activity ◽  
Anti Hiv Agents ◽  
Derivatives Of ◽  
Anti Hiv

scholarly journals Ingenol Derivatives are Highly Potent and Selective Inhibitors of HIV Replication in Vitro

1996 ◽  
Vol 7 (5) ◽  
pp. 230-236 ◽  
Author(s):  
M. Fujiwara ◽  
K. Ijichi ◽  
K. Tokuhisa ◽  
K. Katsuura ◽  
G.-Y.-S. Wang ◽  
...  
Keyword(s):  
Syncytium Formation ◽  
Selective Inhibitor ◽  
Host Cells ◽  
Hiv Replication ◽  
Virus Adsorption ◽  
Mechanism Of Inhibition ◽  
Anti Hiv Agents ◽  
Anti Hiv

Ingenol 3,5,20-triacetate has recently been identified as a highly potent and selective inhibitor of HIV replication in vitro. To evaluate the potential of ingenol derivatives as anti-HIV agents, several ingenol derivatives have been synthesized and investigated for their anti-HIV activities, structure-activity relationships, and possible mechanisms of action. Among the ingenol derivatives, 13-hydroxyingenol-3-(2,3-dimethylbutanoate)-13-dodecanoate (RD4-2138) proved to be a highly potent and selective inhibitor of HIV replication. Its 50% effective concentration for viral replication in MT-4 cells was 0.07-0.5 nM depending on viral strains, including HIV-2. This concentration was approximately 105-fold lower than its cytotoxic threshold. RD4-2138 was also inhibitory to the syncytium formation induced by cocultivation of Molt-4 cells with Molt-4/IIIB cells (Molt-4 cells chronically infected with HIV-1). Some correlation was observed with the ingenol derivatives between their inhibitory effects on HTLV-IIIB replication and surface CD4 expression in MT-4 cells, suggesting that the mechanism of inhibition is in part attributed to the inhibition of virus adsorption through down-regulation of CD4 molecules in the host cells. However, such correlation was not identified between the inhibition of HTLV-IIIB and the activation of protein kinase C. Thus, they might have a potential as effective anti-HIV agents when toxicity in vivo could be elucidated.

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