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Front Cover: 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 (Chem. Eur. J. 38/2018)
Author(s) -
Nikolayevskiy Herman,
Scerba Michael T.,
Deschamps Jeffrey R.,
Appella Daniel H.
Publication year - 2018
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201802620
Subject(s) - mechanism (biology) , chemistry , thioester , human immunodeficiency virus (hiv) , computational biology , combinatorial chemistry , stereochemistry , biochemistry , biology , virology , enzyme , philosophy , epistemology
Mercaptobenzamide thioester SAMT‐247 is a non‐toxic, mutation‐resistant HIV‐1 maturation inhibitor with a unique mechanism of antiviral activity. The lack of an efficient synthesis as well as gaps in the basic understanding of how this molecule functions have hindered preclinical development. NMR spectroscopic analysis of model reactions that mimic the cellular environment answered fundamental questions about the antiviral mechanism and inspired a high‐yielding, scalable, and cost‐effective three‐step synthesis. More information can be found in the Communication by D. H. Appella, et al. on page 9485.