RESUMO
Novel, mesalazine, metronidazole conjugates 6a-e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.
Assuntos
Anti-Inflamatórios/farmacologia , Mesalamina/farmacologia , Metronidazol/farmacologia , Animais , Anti-Inflamatórios/efeitos adversos , Anti-Inflamatórios/química , Indometacina/toxicidade , Mesalamina/efeitos adversos , Mesalamina/química , Metronidazol/efeitos adversos , Metronidazol/química , Camundongos , Estrutura Molecular , Relação Quantitativa Estrutura-Atividade , Úlcera Gástrica/induzido quimicamenteRESUMO
Novel 18- and 20-membered P,N-macrocycles have been obtained stereoselectively by covalent self-assembly of α,ω-bisphosphines, formaldehyde and benzylamine. Alternating SSSS/RRRR or RSSR diastereomers were formed in the row of the 14-, 16-, 18- and 20-membered macrocyclic aminomethylphosphines. For the first time it was demonstrated that the stereochemical result of the reaction depends on the even or odd number of the methylene groups between the two chiral phosphorus atoms in the initial α,ω-bisphosphines.
RESUMO
A hydride and a silyl group of hydrosilane is introduced into 1,3-divinyldisiloxane in the presence of a catalytic amount of (η(5)-C(5)H(5))Fe(CO)(2)Me. Instead of the product expected from the well-known hydrosilylation reaction, the product obtained is that characteristic of dehydrogenative silylation at one vinyl group and hydrogenation at the other vinyl group of 1,3-divinyldisiloxane. Based on deuterium labeling experiments, a catalytic cycle for this new reaction has been proposed.
Assuntos
Compostos de Ferro/química , Silanos/química , Siloxanas/química , Catálise , Hidrogenação , Estrutura MolecularRESUMO
The title compound was synthesised in moderate yield via stereoselective self-assembly of two bisphosphine, four formaldehyde and two primary amine molecules.