I. J. Gerus

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Two pyoverdin-ampicillin conjugates were synthesized and their structures were confirmed by mass spectrometry and NMR spectroscopy. In contrast to ampicillin, the conjugates exhibited high antibacterial activity against Pseudomonas aeruginosa ATCC 15692 and ATCC 27853, effective only against the strain which is using the parent pyoverdin for iron uptake.(More)
Recently, we have shown that new fluorinated analogues of γ-aminobutyric acid (GABA), bioisosters of pregabalin (β-i-Bu-GABA), i.e. β-polyfluoroalkyl-GABAs (FGABAs), with substituents: β-CF3-β-OH (1), β-CF3 (2); β-CF2CF2H (3), are able to increase the initial rate of [3H]GABA uptake by isolated rat brain nerve terminals (synaptosomes), and this effect is(More)
Fluorinated analogs of natural substances take an essential place in the design of new biologically active compounds. New fluorinated analogs of γ-aminobutyric acid, that is, β-polyfluoroalkyl-GABAs (FGABAs), were synthesized with substituents: β-CF3-β-OH (1), β-CF3 (2); β-CF2CF2H (3). FGABAs are bioisosteres of Pregabalin (Lyrica®, Pfizer's blockbuster(More)
1. V. Velter and V. Klingler, Bioorg. Khim., ~, No. 7, 965-981 (1980). 2. V.E. Klusha, Peptides -Regulators of Brain Functions [in Russian], Riga (1984). 3. Pharmacology of Neuropeptides [in Russian], A. V. Val'dman (ed.), Moscow (1982). 4. So BjBkman, S. Castensson, and H. Silvertsson, J. Med. Chem., 22, 931-935 (1979). 5. S. Co Gerson and R. J.(More)
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