Antagonists of Human CCR5 Receptor Containing 4-(Pyrazolyl)piperidine Side Chains. Part 2. Discovery of Potent Selective, and Orally Bioavailable Compounds.

ChemInform ◽  
2004 ◽  
Vol 35 (25) ◽  
Author(s):  
Dong-Ming Shen ◽  
et al. et al.
Keyword(s):  
Side Chains ◽  
Ccr5 Receptor ◽  
Orally Bioavailable ◽  
Human Ccr5

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds

2004 ◽  
Vol 14 (4) ◽  
pp. 941-945 ◽  
Author(s):  
Dong-Ming Shen ◽  
Min Shu ◽  
Christopher A. Willoughby ◽  
Shrenik Shah ◽  
Christopher L. Lynch ◽  
...  
Keyword(s):  
Side Chains ◽  
Ccr5 Receptor ◽  
Orally Bioavailable ◽  
Human Ccr5

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment

2004 ◽  
Vol 14 (4) ◽  
pp. 947-952 ◽  
Author(s):  
Min Shu ◽  
Jennifer L Loebach ◽  
Kerry A Parker ◽  
Sander G Mills ◽  
Kevin T Chapman ◽  
...  
Keyword(s):  
Side Chains ◽  
Sar Studies ◽  
Ccr5 Receptor ◽  
Human Ccr5

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains

2004 ◽  
Vol 14 (4) ◽  
pp. 935-939 ◽  
Author(s):  
Dong-Ming Shen ◽  
Min Shu ◽  
Sander G. Mills ◽  
Kevin T. Chapman ◽  
Lorraine Malkowitz ◽  
...  
Keyword(s):  
Side Chains ◽  
Ccr5 Receptor ◽  
Sar Study ◽  
Human Ccr5

Antiretroviral agents: Focus on Maraviroc for the Treatment of HIV-1-Infected Adults

2010 ◽  
Vol 2 ◽  
pp. CMT.S5420
Author(s):  
SL. Pett ◽  
S. Emery ◽  
AD. Kelleher ◽  
DA. Cooper
Keyword(s):  
Hiv Infection ◽  
Chemokine Receptors ◽  
Hiv Transmission ◽  
Hiv Therapy ◽  
Ccr5 Receptor ◽  
Tick Borne Encephalitis ◽  
Hiv Entry ◽  
Orally Bioavailable ◽  
Hiv Envelope ◽  
Hiv 1

Over a decade has passed since several groups identified the chemokine receptors CXCR4 and CCR5 as key co-receptors for HIV entry. CCR5 is more important in HIV transmission and during the early course of HIV infection. It is also apparent that protection from HIV infection is afforded to those lacking CCR5–-the so called delta-32 homozygotes; in those heterozygous for this mutation, an attenuated course of HIV-infection is observed. Provocatively, those with modified expression of CCR5 are physiologically normal with the exception of poorer outcomes with some of the viral encephalitides specifically West Nile virus and Tick Borne encephalitis. The small molecule, orally-bioavailable CCR5 receptor antagonists, including, maraviroc (MVC), are allosteric inhibitors that lock the CCR5 receptor into a conformation such that the receptor is not able to bind HIV envelope protein; the molecules also variably block intracellular signalling induced by different receptor-binding chemokines. The aims of this review on the CCR5 receptor inhibitors are to summarise information relevant to treatment in individuals with HIV-1 infection. Data from the licensing studies, the side-effect profile and putative long-term risks of CCR5 receptor inhibitor exposure, tropism testing and mechanisms of resistance will be reviewed. The potential for using this class of agent as an immunomodulating agent will be detailed. Given that MVC is the only licensed drug in this class at present and reflecting the greater body of work describing this agent, the majority of information in this review relates to MVC. Last, the authors propose the place of MVC in the hierarchy of HIV therapy and future opportunities for research.

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
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