N²‐Benzyloxycarbonylguan‐9‐yl Acetic Acid Derivatives as HIV‐1 Reverse Transcriptase Non‐Nucleoside Inhibitors with Decreased Loss of Potency Against Common Drug‐Resistance Mutations.

Abstract

Beating the RT mutants: A novel class of N2‐Cbz‐guan‐9‐yl acetic acid derivatives is endowed with anti‐HIV‐1 reverse transcriptase (RT) activity in the low micromolar range. These compounds have improved efficacy towards drug‐resistant RT mutants relative to nevirapine and efavirenz. Their unique scaffold and interesting resistance profiles warrant further development.

PPG Peptide Nucleic Acids that Promote DNA Guanine Quadruplexes

“…Briefly, 2-amino-4,6-dichloropyrimidine-5-carboxyaldehyde was condensed with ethyl hydrazinoacetate followed by protection of the exocyclic amine as a Cbz carbamate. 24 A 2-step hydrolysis was then performed to afford the PPG-acetic acid. This nucleobase acetic acid was then coupled to aminoethyl glycine PNA backbone or (S,S)- trans -cyclopentane PNA backbone, to make aegPNA PPG monomer ( 1 ) and cypPNA PPG monomer ( 2 ), respectively.…”