On December 10, 2015, Behnam, Mira A. M.; Graf, Dominik; Bartenschlager, Ralf; Zlotos, Darius P.; Klein, Christian D. published an article.Name: H-Phg(4-OH)-OH The title of the article was Discovery of Nanomolar Dengue and West Nile Virus Protease Inhibitors Containing a 4-Benzyloxyphenylglycine Residue. And the article contained the following:
The dengue virus (DENV) and West Nile Virus (WNV) NS2B-NS3 proteases are attractive targets for the development of dual-acting therapeutics against these arboviral pathogens. We present the synthesis and extensive biol. evaluation of inhibitors that contain benzyl ethers of 4-hydroxyphenylglycine as non-natural peptidic building blocks synthesized via a copper-complex intermediate. A three-step optimization strategy, beginning with fragment growth of the C-terminal 4-hydroxyphenylglycine to the benzyloxy ether, followed by C- and N-terminal optimization, and finally fragment merging generated compounds with in vitro affinities in the low nanomolar range. The most promising derivative reached Ki values of 12 nM at the DENV-2 and 39 nM at the WNV proteases. Several of the newly discovered protease inhibitors yielded a significant reduction of dengue and West Nile virus titers in cell-based assays of virus replication, with an EC50 value of 3.4 μM at DENV-2 and 15.5 μM at WNV for the most active analog. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Name: H-Phg(4-OH)-OH
The Article related to hydroxyphenylglycine peptide preparation protease inhibitor dengue west nile virus, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Name: H-Phg(4-OH)-OH
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