The reaction of spiro- and dispiro-1,2,4-trioxolane antimalarials with heme has been investigated to provide further insight into the mechanism of action for this important class of antimalarials. A series of trioxolanes with various antimalarial potencies was found to be unreactive in the presence of Fe(III) hemin, but all were rapidly degraded by reduced Fe(II) heme. The major reaction produc...

The intermolecular interactions of metallothionein with nitrogen mustard drugs were studied by molecular dynamics simulations. Previous laboratory experiments have defined selective alkylation of two cysteine residues, and selective binding was proposed to precede alkylation. The present study provides information about accessibility to cysteines based on evaluating the intermolecular energies ...

The paper provides a comprehensive review of the base-catalysed C3-alkylation of N-unprotected-3-monosubstituted oxindoles. Based on a few, non-systematic studies described in the literature using butyllithium as the deprotonating agent, an optimized method has now been elaborated, via the corresponding lithium salt, for the selective C3-alkylation of this family of compounds. The optimal exces...

vapor-phase methylation of toluene using methanol and its isopropylation with 2-propanol has been investigated ina down flow reactor under atmospheric conditions using n2 carrier over a series of surface modified andunmodified zsm-5 (si/al= 60-170) loaded with h3po4, differing in the external surface treatment of the zeolites.the feed molar ratios of toluene/methanol and toluene/2-propanol were...

ammonium monovanadate (nh4vo3) has been devoted as an efficient, commercially available, eco-friendly and reusable catalyst for the synthesis of bis(indolyl)methanes (bims), oxindole derivatives and also michael adducts of indoles at 50 °c under solvent-free conditions. the reusability of this solid acid catalyst in addition with its selectivity has also been examined.

Chitosan, a natural polysaccharide, has been widely used as biomaterial, especially for hemostasis. However, hemostatic materials processed from pure chitosan have limited effect and are extremely unstable in some cases; chemical modification is therefore needed to improve the properties of chitosan. Through reactions with hydroxyl amino groups macromolecules, such alkylation, carboxylation, qu...

Vapor-phase methylation of toluene using methanol and its isopropylation with 2-propanol has been investigated ina down flow reactor under atmospheric conditions using N2 carrier over a series of surface modified andunmodified ZSM-5 (Si/Al= 60-170) loaded with H3PO4, differing in the external surface treatment of the zeolites.The feed molar ratios of toluene/methanol and toluene/2-propanol were...

Previous work has shown that alkylation of DNA by the antitumor agent leinamycin (1) is potentiated by reaction of the antibiotic with thiols. Here, it is shown that other soft nucleophiles such as cyanide and phosphines can also trigger DNA alkylation by leinamycin. Overall, the results suggest that reactions of cyanide and phosphines with leinamycin produce the oxathiolanone intermediate (2),...

Conformational preferences of the pyrrolidine ring in nucleotide analogs 7-14 were investigated by means of NMR and molecular modeling. The effect of the relative configuration of hydroxy and nucleobase substituents as well as the effect of the alkylation or acylation of the pyrrolidine nitrogen atom on the conformation of the pyrrolidine ring were studied. The results of a conformational analy...

Economic and environmentally friendly bio-mimetic one-pot three and four-component Knoevenagel-hydrogenation (K-H), five-component Knoevenagel-hydrogenation-alkylation (K-H-A) and six-component Knoevenagel-hydrogenation-alkylation-Huisgen cycloaddition (K-H-A-HC) reactions of aldehydes, CH-acids, o-phenylenediamine, alkyl halides and azides using proline, proline-metal carbonate and proline-met...