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Reaction Kinetics Direct a Rational Synthesis of an HIV-1 Inactivator of Nucleocapsid Protein 7 and Provide Mechanistic Insight Into Cellular Metabolism and Antiviral Activity

Herman Nikolayevskiy, Michael T Scerba, Jeffrey R Deschamps, Daniel H Appella

Chemistry. 2018 Jul 5;24(38):9485-9489.

PMID: 29653024

Abstract:

Mercaptobenzamide thioester SAMT-247 is a non-toxic, mutation-resistant HIV-1 maturation inhibitor with a unique mechanism of antiviral activity. NMR spectroscopic analyses of model reactions that mimic the cellular environment answered fundamental questions about the antiviral mechanism and inspired a high-yielding (64 % overall), scalable (75 mmol), and cost-effective ($4 mmol-1 ) three-step synthesis that will enable additional preclinical evaluation.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP850715592 SAMT-247 SAMT-247 850715-59-2 Price
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