Myrosinase, a thioglucoside glucohydrolase, is the only enzyme able to hydrolyse glucosinolates, a unique family of molecules bearing an anomeric O-sulfated thiohydroximate function. Non-hydrolysable myrosinase inhibitors have been devised and studied for their biological interaction. Diverse modifications of the O-sulfate moiety did not result in a significant inhibitory effect, whereas replacing the D-glucopyrano residue by its carba-analogue allowed inhibition to take place. X-Ray experiments carried out after soaking allowed for the first time inclusion of a non-hydrolysable inhibitor inside the enzymatic pocket. Structural tuning of the aglycon part in its pocket is being used as a guide for the development of simplified and more potent inhibitors.
The behaviour of an acridine-functionalized calix [4]arene at the interface between two immiscible electrolyte solutions (ITIES) is reported. Molecular modelling showed that the acridine-calix[4]arene has regions of significant net positive charge spread throughout the protonated acridine moieties, consistent with it being able to function as an anion ionophore.The presence of this compound in the organic phase facilitated the transfer of aqueous phase electrolyte ions. Upon addition of double stranded DNA to the aqueous phase, the transfer of electrolyte anions was diminished, due to DNA binding to the acridine moiety at the ITIES. The behaviour provides a basis for DNA hybridization detection using electrochemistry at the ITIES.
Deprotection O 0345Mild and Selective Deprotection of Carbamates with Bu 4 NF. -The cleavage of various aliphatic, allylic, benzylic, and phenyl carbamates, protecting different kinds of nitrogen, by Bu4NF in THF is studied. Phenyl carbamates are very easily cleaved except for secondary aromatic amines. For tryptamine derivatives (IX) and (XI) bearing two protected nitrogen atoms, selective cleavage is observed. The presence of an aliphatic or vinylic methyl ester function seems to inhibit the carbamate cleavage and hydrolysis to the corresponding acids occurs. -(JACQUEMARD, U.; BENETEAU, V.; LEFOIX, M.; ROUTIER, S.; MEROUR, J.-Y.; COUDERT*, G.; Tetrahedron 60
The synthesis of a pyrazolo[1,5-a]-1,3,5-triazine C-nucleoside (dA(PT)), designed to form two hydrogen bonds with a complementary dT residue, is reported. Oligonucleotides including this dA nucleoside analogue possess base-pairing properties similar to those of the parent oligonucleotide. This dA nucleoside analogue is more resistant to acid-catalyzed hydrolysis than dA.
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