Synthesis and anti-HIV-1 evaluation of some novel MC-1220 analogs as non-nucleoside reverse transcriptase inhibitors
LODDO, ROBERTA;LA COLLA, PAOLO
2016-01-01
Abstract
Some novel MC-1220 analogs were synthesized by condensation of 4,6-dichloro-N-methylpyrimidin-2-amine derivatives (1a,b and 15) and/or 4-chloro-6-methoxy-N,N,5-trimethylpyrimidin-2-amine (2a) with the sodium salt of 2,6-difluorophenylacetonitrile followed by treatment with aqueous sodium hydroxide in methanol, alkylation, reduction, halogenation, and/or acidic hydrolysis. All synthesized compounds were evaluated for their activity against HIV-1. The most active compound in this study was compound 7, which showed activity against HIV-1 comparable to that of MC-1220. The only difference in structure between compound 7 and MC-1220 is a fluoro atom instead of a CH3 groupFile | Size | Format | |
---|---|---|---|
Loksha_et_al-2016-Archiv_der_Pharmazie-3.pdf Solo gestori archivio
Type: versione editoriale
Size 723.07 kB
Format Adobe PDF
|
723.07 kB | Adobe PDF | & nbsp; View / Open Request a copy |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.