Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors

[tetano]

Eur J Med Chem. 2014 Jun 26;83C:466-473. doi: 10.1016/j.ejmech.2014.06.059. [Epub ahead of print]
Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
Lou J1, Yang X1, Rao Z1, Qi W1, Li J1, Wang H1, Li Y1, Li J1, Wang Z1, Hu X1, Liu P2, Hong X1.
Author information
Abstract

A series of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives were prepared to evaluate their ability of inhibiting neuraminidase (NA) of influenza A virus. All the compounds were synthesized in good yields starting from aldehyde by using a suitable synthetic strategy, which showed moderate inhibitory activity against influenza A NA. Compound 6g exhibited the strongest inhibitory activity against influenza virus A NA (IC50 = 17.64 μM), which indicated pyrimidine ring could be used as a core structure to design novel influenza NA inhibitors.

Copyright ? 2014. Published by Elsevier Masson SAS.
KEYWORDS:

6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives; Anti-influenza; Neuraminidase inhibitors; SAR

PMID:
24992074
[PubMed - as supplied by publisher]

http://www.ncbi.nlm.nih.gov/pubmed/24992074