Selected papers

Design and Synthesis of Fluorescent Acyclic Nucleoside Phosphonates as Potent Inhibitors of Bacterial Adenylate Cyclases
Design and Synthesis of Fluorescent Acyclic Nucleoside Phosphonates as Potent Inhibitors of Bacterial Adenylate Cyclases
ChemMedChem 11 (22): 2534-2546 (2016)
Bordetella pertussis adenylate cyclase toxin (ACT) and Bacillus anthracis edema factor (EF) are key virulence factors with adenylate cyclase (AC) activity that substantially contribute to the pathogenesis of whooping cough and anthrax, respectively. There is an urgent need to develop potent and selective inhibitors of bacterial ACs with prospects for the development of potential antibacterial therapeutics and to study their molecular interactions with the target enzymes. Novel fluorescent 5‐chloroanthraniloyl‐substituted acyclic nucleoside phosphonates (Cl‐ANT‐ANPs) were designed and synthesized in the form of their diphosphates (Cl‐ANT‐ANPpp) as competitive ACT and EF inhibitors with sub‐micromolar potency (IC50 values: 11–622 nm). Fluorescence experiments indicated that Cl‐ANT‐ANPpp analogues bind to the ACT active site, and docking studies suggested that the Cl‐ANT group interacts with Phe306 and Leu60. Interestingly, the increase in direct fluorescence with Cl‐ANT‐ANPpp having an…

Latest publications

Xanthine-based acyclic nucleoside phosphonates with potent antiviral activity against varicella-zoster virus and human cytomegalovirus
Antiviral Chemistry and Chemotherapy 26: 1-13 (2018)
Design and Synthesis of Fluorescent Acyclic Nucleoside Phosphonates as Potent Inhibitors of Bacterial Adenylate Cyclases
ChemMedChem 11 (22): 2534-2546 (2016)
Efficient one-pot synthesis of polysubstituted 6-[(1H-1,2,3-triazol-1-yl)methyl]uracils through the “click” protocol
Collection of Czechoslovak Chemical Communications 76 (9): 1121-1131 (2011)
The synthesis of the 8-C-substituted 2,6-diamino-9-[2-(phosphonomethoxy)ethyl]purine (PMEDAP) derivatives by diverse cross-coupling reactions
Canadian Journal of Chemistry 89 (4): 488-489 (2011)