Synthesis and antimicrobial activity evaluation of novel phosphorylated derivatives of zidovudine

S Reddy, V Koteswara Rao, K Venkataramana, C Suresh Reddy, S Ghosh, C Naga Rju
2010 Der Pharma Chemica   unpublished
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
more » ... 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.
fatcat:bcz7uwvolbafro6x6izmqio74q