Add time:07/16/2019         Source:sciencedirect.com

A series of peptides containing N-(2,3-dihalopropyl)-glycine or alanine residues has been prepared as potential suicide substrates of the HIV pol-protease or as enzyme-activated prodrugs. Halogenation of unsaturated N-allyl peptide precursors in dichloromethane occurs with participation of a neighboring amide group and leads to halohydrins instead of the expected dihalides. Use of X2/ LiX/HOAc conditions gives the desired dihalogenated derivatives. These functionalized substrate analogs are not inhibitors of the enzyme. However, Boc-Ala-Phe-N-(2,3-dihalogenopropyl)-Gly-Ile-Val-OMe (halogen= Br and Cl) inhibit the cytopathic effect induced by HIV-1 in CEM cell cultures and the reverse transcriptase activity in cell culture supernatants. The corresponding unsaturated N-allyl precursor also displays an antiviral effect.

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