GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection . To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 ( CXCR4 ) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1 . It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection .
Products | Products > Disease Areas > Infection | Products > Signaling Pathways > Anti-infection | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > GPCR/G Protein | Products > Research Areas > Infection | Products > Signaling Pathways > HIV | Products > Signaling Pathways > CXCR
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