Synthesis and antimicrobial activity evaluation of novel phosphorylated derivatives of zidovudine
release_bcz7uwvolbafro6x6izmqio74q
by
S Reddy,
V Koteswara Rao,
K Venkataramana,
C Suresh Reddy,
S Ghosh,
C Naga Rju
2010
Abstract
A series of novel phosphorylated derivatives of zidovudine (5-15) were synthesized in two step process with high yields. In the first step zidovudine (1) was reacted with bis(2-chloroethyl) phosphoramidicdichloride/4-nitrophenylphosphorodichloridate/4-chloro phenyl phosphorodi-chloridate in presence of triethylamine (TEA) in dry tetrahydrofuran (THF) to yield the intermediates (2-4). They were further reacted with various compounds like monopotassium dihydrogenphosphate and amino acid esters to obtain the title compounds 5-15. The title compounds showed promising antimicrobial activity and it was greatly influenced by the presence of different bio-active groups at phosphorus.
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