Salt or a cocrystal? Predicting the structure of multicomponent solids with a hydrogen bond
13 July 2022
A large number of drugs currently on the market contain an active ingredient in a multicomponent solid form. The biologically active substance itself often has an alkaline…
National Institute of Virology and Bacteriology to help manage future epidemics
21 June 2022
The COVID-19 pandemic, which broke out more than two years ago, clearly demonstrated the critical importance of science and research. It also revealed how important active…
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Synthesis and anti-trypanosomal evaluation of novel N-branched acyclic nucleoside phosphonates bearing 7-aryl-7-deazapurine nucleobase
European Journal of Medicinal Chemistry 239: 114559 (2022)
A series of novel 7-aryl-7-deazaadenine-based N-branched acyclic nucleoside phosphonates (aza-ANPs) has been prepared using the optimized Suzuki cross-coupling reaction as the key synthetic step. The final free phosphonates 15a-h were inactive, due to their inefficient transport across cell membranes, but they inhibited Trypanosoma brucei adenine phosphoribosyltransferase (TbrAPRT1) with Ki values of 1.7–14.1 μM. The corresponding phosphonodiamidate prodrugs 14a-h exhibited anti-trypanosomal activity in the Trypanosoma brucei brucei cell-based assay with EC50 values in the range of 0.58–6.8 μM. 7-(4-Methoxy)phenyl-7-deazapurine derivative 14h, containing two phosphonate moieties, was the most potent anti-trypanosomal agent from the series, with EC50 = 0.58 μM and SI = 16. Finally, phosphonodiamidate prodrugs 14a-h exerted low micromolar cytotoxicity against leukemia and/or cancer cell lines tested.
Photochemical synthesis of pink silver and its use for monitoring peptide nitration via surface enhanced Raman spectroscopy (SERS)
Amino Acids 2022: Early View
Unified Total Synthesis of Diverse Meroterpenoids from Ganoderma applanatum
Organic Letters 24 (25): 4552–4556 (2022)
Regio- and Diastereoselective 1,3-Dipolar Cycloadditions of 1,2,4-Triazin-1-ium Ylides: a Straightforward Synthetic Route to Polysubstituted Pyrrolo[2,1-f][1,2,4]triazines
ACS Omega 7 (24): 21233–21238 (2022)