Results 151 to 160 of about 6,286 (187)

Practical Asymmetric Synthesis of RO5114436, a CCR5 Receptor Antagonist

Organic Process Research & Development, 2010
A practical asymmetric synthesis of a 3,7-diazabicyclo[3.3.0]octane derivative (1), a representative of a new class of potent CCR5 receptor antagonists, is described. The benzylamine stereogenic center of 1 was introduced by a ruthenium-catalyzed asymmetric reductive amination using (R)-MeOBIPHEP as ligand.
Xiaojun Huang, Erin O’Brien, Felicia Thai, Gary Cooper   +3 more
openaire   +1 more source

Allosteric mechanism of an oximino‐piperidino‐piperidine antagonist for the CCR5 chemokine receptor

Chemical Biology & Drug Design, 2019
AbstractThe first step for the HIV‐1 virus infecting host cell is bound with the CCR5 chemokine receptor. A set of allosteric inhibitors of oximino‐piperidino‐piperidine antagonists for CCR5 chemokine receptor was discovered. However, the allosteric mechanism of these inhibitors is still unsolved.
Yangpeng Zhang, Hai‐Feng Chen
openaire   +2 more sources

ChemInform Abstract: CCR5 Receptor Antagonist

ChemInform, 2011
AbstractReview: 39 refs.
openaire   +1 more source

Practical Convergent Laboratory-Scale Synthesis of a CCR5 Receptor Antagonist

Organic Process Research & Development, 2011
An efficient laboratory-scale synthesis has been developed for the selective CCR5 antagonist 1. The convergent route has a longest linear sequence of nine steps (15 steps overall), and has overall yields of 18–25%. The route has enabled the preparation of 550 g of 1.
Jason B. Crawford, Gang Chen, Bryon Carpenter, Trevor Wilson, Jenny Ji, Renato T. Skerlj, Gary J. Bridger   +6 more
openaire   +1 more source

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains

Bioorganic & Medicinal Chemistry Letters, 2003
The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacokinetics.
Christopher L, Lynch, Christopher A, Willoughby, Jeffrey J, Hale, Edward J, Holson, Richard J, Budhu, Amy L, Gentry, Keith G, Rosauer, Charles G, Caldwell, Ping, Chen, Sander G, Mills, Malcolm, MacCoss, Scott, Berk, Liya, Chen, Kevin T, Chapman, Lorraine, Malkowitz, Martin S, Springer, Sandra L, Gould, Julie A, DeMartino, Salvatore J, Siciliano, Margaret A, Cascieri, Anthony, Carella, Gwen, Carver, Karen, Holmes, William A, Schleif, Renee, Danzeisen, Daria, Hazuda, Joseph, Kessler, Janet, Lineberger, Michael, Miller, Emilio A, Emini   +29 more
openaire   +2 more sources

Elucidation of Binding Sites of Dual Antagonists in the Human Chemokine Receptors CCR2 and CCR5

Molecular Pharmacology, 2009
Design of dual antagonists for the chemokine receptors CCR2 and CCR5 will be greatly facilitated by knowledge of the structural differences of their binding sites. Thus, we computationally predicted the binding site of the dual CCR2/CCR5 antagonist N-dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzohepten-8-yl] carbonyl]amino]benzyl]tetrahydro ...
Spencer E, Hall, Allen, Mao, Vicky, Nicolaidou, Mattea, Finelli, Emma L, Wise, Belinda, Nedjai, Julie, Kanjanapangka, Paymann, Harirchian, Deborah, Chen, Victor, Selchau, Sofia, Ribeiro, Sabine, Schyler, James E, Pease, Richard, Horuk, Nagarajan, Vaidehi   +14 more
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Developing clinical role of a CCR5 co-receptor antagonist in HIV-1 infection

Expert Opinion on Pharmacotherapy, 2008
Maraviroc is the only approved CCR5 coreceptor antagonist on the market for treatment of HIV-1 infection. It uses a previously untargeted step in the HIV-1 replication cycle necessary for viral entry into the host cell.This review will describe and evaluate recent clinical literature regarding maraviroc, focusing on safety, efficacy, and mechanisms of ...
David J, Caldwell, Jeffery D, Evans
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DEVELOPMENT OF ANTAGONISTS TARGETING CHEMOKINE RECEPTOR CCR5 AND THE CHEMOKINE RECEPTOR CCR5 - MU OPIOID RECEPTOR HETERODIMER

2013
VCU Theses and ...
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1,3,4‐Trisubstituted Pyrrolidine CCR5 Receptor Antagonists: Modifications of Arylpropylpiperidine Side Chains.

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Christopher L. Lynch, et al. et al.
openaire   +1 more source

Identification of Human Liver Cytochrome P450 Enzymes Involved in Biotransformation of Vicriviroc, a CCR5 Receptor Antagonist

Drug Metabolism and Disposition, 2007
Vicriviroc (SCH 417690), a CCR5 receptor antagonist, is currently under investigation for the treatment of human immunodeficiency virus infection. The objective of this study was to identify human liver cytochrome P450 enzyme(s) responsible for the metabolism of vicriviroc.
Anima, Ghosal, Ragu, Ramanathan, Yuan, Yuan, Neil, Hapangama, Swapan K, Chowdhury, Narendra S, Kishnani, Kevin B, Alton   +6 more
openaire   +2 more sources