Yan, Linjie published the artcileDesign, synthesis and evaluation of 2′-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents, Recommanded Product: 3-Pentanol, the main research area is alkylaminopyrrolopyrimidinylethynyl tetrahydrofuranylmethoxyphenoxyphosphorylaminopropanoate preparation diastereoselective antiviral SAR pharmacokinetic; Antiviral; Enterovirus; NITD008; Nucleoside/nucleotide inhibitor.
A series of phosphoamidate derivatives I [R1 = Me, iso-Bu, cyclohexyl etc.; R2 = H, Me, benzyl etc.] (NITD008) were synthesized and evaluated for their in-vitro antiviral activities against the enteroviruses EV71 and EV-D68. The phosphoamidate containing I [R1 = n-hexyl; R2 = Me] a hexyl ester of L-alanine exhibited the most promising activity against EV71 (IC50 = 0.13 ± 0.08 μM) and were 4-times more potent than NITD008. Meanwhile, the derivative containing a cyclohexyl ester of L-alanine I [R1 = cyclohexyl; R2 = Me] exhibited the most potent activity with high selectivity index against both EV71 (IC50 = 0.19 ± 0.27 μM, SI = 117.00) and EV-D68 (IC50 = 0.17 ± 0.16 μM, SI = 130.76), which were both higher than that of NITD008. The results indicated that the phosphoamidate I [R1 = cyclohexyl; R2 = Me] were the most promising candidate for further development as antiviral agents for the treatment of both EV71 and EV-D68 infection.
European Journal of Medicinal Chemistry published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 584-02-1 belongs to class alcohols-buliding-blocks, name is 3-Pentanol, and the molecular formula is C5H12O, Recommanded Product: 3-Pentanol.
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