Neoglycopeptide dendrimer libraries as a source of lectin binding ligands

[structure: see text] A 15 625-membered peptide dendrimer combinatorial library was acylated with an alpha-C-fucosyl residue at its four N-termini and screened for binding to fucose-specific lectins. Dendrimer FD2 (Fuc-alpha-CH2CO-Lys-Pro-Leu)4(Lys-Phe-Lys-Ile)2Lys-His-Ile-NH2 was identified as a potent ligand against Ulex europaeus lectin UEA-I (IC50 = 11 microM) and Pseudomonas aeruginosa lectin PA-IIL (IC50 = 0.14 microM).     

Chirality induction and protonation-induced molecular motions in helical molecular strands

The long oligopyridinedicarboxamide strand 9, containing 15 heterocyclic rings has been synthesized and its helical structure determined by X-ray crystallography. It was shown that the shorter analogue 6 displays induced circular dichroism and amplification of induced chirality upon dissolution in an optically active solvent, diethyl-L-tartrate. A novel class of helical foldamers was prepared, strands 14-16, based on two oligopyridine carboxamide segments linked through a L-tartaric acid derived spacer. These tartro strands display internal chirality induction as well as chirality amplification. NMR spectroscopy (on 8 and 9) and circular dichroism (on 16) studies show that the oligopyridine carboxamide strands undergo reversible unfolding/folding upon protonation. The protonation-induced unfolding has been confirmed by X-ray crystallographic determination of the molecular structure of the extended protonated heptameric form 8(+). The molecular-scale mechano-chemical motions of the protonation-induced structural switching consist of a change of the length of the molecule, from 6 angstroms (6, coiled form) to 29 angstroms (8(+), uncoiled form) for the heptamer and from 12.5 angstroms (9, coiled form, X-ray structure) to 57 angstroms (9(+), uncoiled form, from modeling) for the pentadecamer. Similar unfolding/folding motional processes take place in the L-tartro strands 15 and 16 upon protonation/deprotonation, with loss of helicity-induced circular dichroism on unfolding as shown for the protonated form 16(+).     

A study of the feasibility of conducting the ELISE and EXL experiments at the ITEP accelerator complex

We report the results of a study into the feasibility of conducting the ELISE and EXL experiments on collisions of nuclei of radioactive fragments with electrons at the Institute for Theoretical and Experimental Physics (ITEP). A scheme for uranium ion acceleration in the ITEP accelerator complex is chosen, and it is shown that uranium ions may be accelerated with an intensity of ～1 × 10¹¹ ions/s as soon as the complex is modified and a new injector is constructed. The basic parameters of the modified complex are given, and a layout diagram indicating the positions of the target that serves to produce radioactive fragments, the separator, and the storage rings (CR, RESR, NESR, and ER) at the ITEP site is presented.     

Features of the (2+3)-cycloaddition of trifluoroacetonitrile oxide

The (2+3)-cycloaddition of trifluoroacetonitrile oxide is a function of the donor and steric properties of dipolarophiles and usually proceeds regiospecifically. A significant temperature effect was found for the cycloaddition of trifluoroacetonitrile oxide to dipolarophiles with low donor capacity.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 972–974, July, 1989.     

C-alkylation of N-alkylanilines by polyfluoroketones

Conclusions Conditions were found for the mild C-alkylation of secondary and tertiary aromatic amines by hexafluoroacetone and methyl trifluoropyruvate. The regiospecific formation of the products of C(4)-alkylation was demonstrated.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 4, pp. 931–934, April, 1985.     

Synthesis of α-(4-hydroxyphenyl)-β,β,β-trifluoro-α-alanine derivatives

2,6-Dimethyl- and 2,6-dimethoxy-α-methoxycarbonyl-α-trifluoromethyl-p-methylenequinones have been synthesized. These compounds easily react with ammonia, morpholine, andp-toluidine to afford the corresponding α-(4-hydroxyphenyl)-β,β,β-trifluoro-α-alanine derivatives.     

α-Methoxycarbonyl-containing polyflouoalkylsulfenyl chlorides

New -methoxycarbon-containingy polyflnoroalkylsulfenyl chlorides were obtained. Reactions of sulfenyl chlorides containing primary, secondary and tertiary -methoxycarbonyl polyfluoroalkyl groups at the sulfur atom with some unsaturated, carbonyl, arromatic, and heteroaromatic compounds were studied.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya No 7. pp 1745–1752. July, 1996.