New insight into nucleo α-amino acids - Synthesis and SAR studies on cytotoxic activity of β-pyrimidine alanines.

Three series of the β-pyrimidine alanines, including willardiine - a naturally occurring amino acid, were prepared from the l-serine-derived sulfamidates. Compounds 3b, 4a and 4b demonstrated antiproliferative activity toward the studied cancer cell lines, albeit the effect of these compounds on human brain astrocytoma MOG-G-CCM cells was more significant than on human neuroblastoma SK-N-AS cells. The cytosine analog of willardiine, compound 4b, reduced viability of MOG-G-CCM cells with EC = 36 ± 2 μM, more effectively than AMPA antagonist GYKI 52466.

Potential bioisosteres of β-uracilalanines derived from 1H-1,2,3-triazole-C-carboxylic acids.

The 1H-1,2,3-triazole-originated derivatives of willardiine were obtained by: (i) construction of the 1H-1,2,3-triazole ring in 1,3-dipolar cycloaddition of the uracil-derived azides and the carboxylate-bearing alkynes or α-acylphosphorus ylide, or (ii) N-alkylation of the uracil derivative with the 1H-1,2,3-triazole-4-carboxylate-derived mesylate. The latter method offered: (i) reproducible results, (ii) a significant reduction of amounts of auxiliary materials, (iii) reduction in wastes and (iv) reduction in a number of manual operations required for obtaining the reaction product. Compound 6a exhibited significant binding affinity to hHS1S2I ligand-binding domain of GluR2 receptor (EC = 2.

Corrigendum: Cross-Talk between and Other Staphylococcal Species via the Quorum Sensing System.

[This corrects the article on p. 1733 in vol. 7, PMID: 27877157.

Corrigendum: Cross-Talk between and Other Staphylococcal Species via the Quorum Sensing System.

[This corrects the article on p. 1733 in vol. 7, PMID: 27877157.

Cross-Talk between and Other Staphylococcal Species via the Quorum Sensing System.

Staphylococci are associated with both humans and animals. While most are non-pathogenic colonizers, is an opportunistic pathogen capable of causing severe infections. virulence is controlled by the quorum sensing system responding to secreted auto-inducing peptides (AIPs) sensed by AgrC, a two component histidine kinase.