Results 141 to 150 of about 6,286 (187)

CCR5 receptor antagonists: Discovery and SAR of novel 4-hydroxypiperidine derivatives

Bioorganic and Medicinal Chemistry Letters, 2007
The guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde, 1, with an IC(50) of 840 nM against the CCR5 receptor was identified using high-throughput screening. Optimization efforts led to the discovery of a novel piperidine series of CCR5 antagonists.
Gary B Phillips
exaly   +3 more sources

Docking and CoMFA study on novel human CCR5 receptor antagonists

Medicinal Chemistry Research, 2012
The CC-chemokine receptor 5 (CCR5), a membrane protein belonging to the G protein-coupled receptor super-family, has been identified as an essential co-receptor for HIV entry into the cells. Small molecules were used to inhibit HIV entry by targeting CCR5.
Jahan Ghasemi, Maryam Nouri, Ghasemi Jahan B   +2 more
exaly   +2 more sources

Three-dimensional quantitative structure–activity relationship analyses of piperidine-based CCR5 receptor antagonists

Bioorganic and Medicinal Chemistry, 2004
The CCR5 chemokine receptor has recently been found to play a crucial role in the viral entry stage of HIV infection and has therefore become an attractive potential target for anti-HIV therapeutics. On the other hand, the lack of CCR5 crystal structure data has impeded the development of structure-based CCR5 antagonist design.
N Sukumar
exaly   +3 more sources

4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents

Bioorganic and Medicinal Chemistry Letters, 2009
A series of 4,4-disubstituted cyclohexylamine based CCR5 antagonists has been designed and synthesized. Their antiviral structure-activity relationship has been extensively explored.
Wieslaw Kazmierski, MAOSHENG Duan, Robert Ferris   +2 more
exaly   +3 more sources

Small Molecule Antagonists of the Chemokine Receptor CCR5

Current Topics in Medicinal Chemistry, 2010
This review will focus on the discovery and clinical development of small molecule antagonists of CCR5 for the treatment of HIV-1/AIDS, as well as for the potential treatment of inflammatory diseases. In particular, we will focus on the specific medicinal chemistry problems that were faced during the discovery of the molecules.
Rémy C, Lemoine, Jutta, Wanner
openaire   +2 more sources

Isolation and Structure of Antagonists of Chemokine Receptor (CCR5)

Journal of Natural Products, 2004
Human CCR5 is a G-coupled receptor that binds to the envelope protein gp120 and CD4 and mediates the HIV-1 viral entry into the cells. The blockade of this binding by a small molecule receptor antagonist could lead to a new mode of action agent for HIV-1 and AIDS. Screening of natural product extracts led to the identification of anibamine (1), a novel
Hiranthi, Jayasuriya, Kithsiri B, Herath, John G, Ondeyka, Jon D, Polishook, Gerald F, Bills, Anne W, Dombrowski, Marty S, Springer, Sal, Siciliano, Lorraine, Malkowitz, Manuel, Sanchez, Ziqiang, Guan, Suroojnauth, Tiwari, Dennis W, Stevenson, Robert P, Borris, Sheo B, Singh   +14 more
openaire   +2 more sources

Allosteric effects of antagonists on signalling by the chemokine receptor CCR5

Biochemical Pharmacology, 2007
Antagonists of the chemokine receptor, CCR5, may provide important new drugs for the treatment of HIV-1. In this study we have examined the mechanism of action of two functional antagonists of the chemokine receptor CCR5 (UK-396,794, UK-438,235) in signalling and internalisation assays using CHO cells expressing CCR5. Both compounds were potent inverse
Ben, Haworth, Hong, Lin, Mark, Fidock, Pat, Dorr, Philip G, Strange   +4 more
openaire   +2 more sources

Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor

International Immunopharmacology, 2007
The species selectivity of four structurally different compounds, SCH-351125, E-913, TAK-779 and UK-427857 has been examined using cloned human, rhesus, and mouse CCR5 receptors. SCH-351125 and E-913 potently inhibited the binding of [125I]-CCL3 to human CCR5, but their inhibitory activities against rhesus CCR5 were more than 10-fold weaker.
Yuji, Saita, Mitsuhiro, Kondo, Yasuaki, Shimizu   +2 more
openaire   +2 more sources

Structure-Activity Relationship Studies: M2 and CCR5 Receptor Antagonists

Current Topics in Medicinal Chemistry, 2003
A wide range of neurotransmitters, polypeptides and inflammatory mediators transduce their signals into the interior of cell by specific interactions with cell-surface receptors that are coupled to G-protein. The most familiar G-protein-coupled receptors are muscarinic receptors, adrenergic receptors, dopaminergic receptors and opioid receptors.
Craig D, Boyle, Anandan, Palani
openaire   +2 more sources

Maraviroc: A CCR5-receptor antagonist for the treatment of HIV-1 infection

Clinical Therapeutics, 2008
The emergence of viral resistance is one of the greatest challenges in the treatment of HIV infection. Maraviroc is the first member of a new class of antiretroviral medications, the CCR5-receptor antagonists. It is approved by the US Food and Drug Administration (FDA) for use in combination with other antiretroviral agents in treatment-experienced ...
Sharon S, Lieberman-Blum, Horatio B, Fung, Juan C, Bandres   +2 more
openaire   +2 more sources