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Synthesis and Anti‐HIV‐1 Evaluation of Some Novel MC‐1220 Analogs as Non‐Nucleoside Reverse Transcriptase Inhibitors
Author(s) -
Loksha Yasser M.,
Pedersen Erik B.,
Loddo Roberta,
La Colla Paolo
Publication year - 2016
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201600008
Subject(s) - chemistry , amine gas treating , hydrolysis , halogenation , sodium hydroxide , methanol , alkylation , stereochemistry , medicinal chemistry , nucleoside , aqueous solution , chemical synthesis , organic chemistry , in vitro , biochemistry , catalysis
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 CH 3 group.
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