Search results for "derivati"

Über Umsetzungen an Poly-p-lithiumstyrol 2. Mitt. Derivate des poly-p-vinyl-di- und Triphenylmethans

1959

Das kurzlich von uns beschriebene Poly-p-lithiumstyrol stellt eine sehr reaktionsfahige makromolekulare metallorganische Verbindung dar. Es wird uber einige Umsetzungen mit Carbonylverbindungen berichtet. Die Reaktion mit Benzaldehyd und einigen p-substituierten Benzaldehyden fuhrt mit hohen Umsetzungsgraden zu Polyvinyldiphenylmethylcarbinolen. Die Reaktion mit Benzophenon liefert Polyvinyltriphenylmethylcarbinol. Diese Verbindung ist in konz. Schwefelsaure loslich als polymeres Analogon des Triphenylmethylkations, was aus der Untersuchung der Absorptionsspektren folgt. Mit MICHLERS Keton last sich ein polymeres Derivat des Malachitgruns darstellen, dessen spektroskopische, Untersuchung in…

Synthesis, antiproliferative activity, and mechanism of action of new benzamido derivatives

2011

The cinnamoyl anthranilamides represent a class of biological active substances of great importance in medicinal chemistry. Moreover, despite their wide range of biological activities, a review of the literature revealed that no anticancer activity is described for this kind of substances. Starting from the 2-cinnamamido-5-iodobenzamide, resulted able to inhibit the leukemic cell line K-562 proliferation with a percent of inhibition of 74% at 10M concentration, we undertake the following structural modifications on cinnamamidobenzamide skeleton: the introduction of various substituents both on the benzamido and the cinnamamido moieties, the substitution of olefinic bond with the ethane, et…

Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis

2018

Abstract: Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence, there is a need to identify new molecular scaffolds and targets as potential therapeutics for the treatment of this disease. We report a small series of 1,2‐substituted‐1H‐benzo[d]imidazole derivatives (9ad) showing affinity in the submicromolar range (Ki = 0.150.69 μM) toward Leishmania mexicanaCPB2.8ΔCTE, one of the more promising targets for antileishmanial drug design. The compounds confirmed activity in vitro against intrace…

Crystal structure of 5-(5,6-dihydrobenzo[4,5]imidazo[1,2-c]quinazolin-6-yl)-2-methoxyphenol

2015

In the molecule of the title compound, C21H17N3O2, the 5,6-dihydrobenzimidazo[1,2-c]quinazoline moiety is disordered over two orientations about a pseudo-mirror plane, with a refined occupancy ratio of 0.863 (2):0.137 (2). The dihedral angles formed by the benzimidazole ring system and the benzene ring of the quinazoline group are 14.28 (5) and 4.7 (3)° for the major and minor disorder components, respectively. An intramolecular O—H...O hydrogen bond is present. In the crystal, molecules are linked by O—H...N hydrogen bonds, forming chains running parallel to [10-1].

The anti-inflammatory properties of tiotropium

2018

N-valproyl-aminoacids as new potential antiepileptic drugs: Synthesis, characterization and in vitro studies on stability

2015

Epilepsy, affecting at least 50 million persons worldwide, is one of the most common neurological disorders. Despite the significant advances in understanding epileptogenic mechanisms and in counteracting their pathological consequences, this clinical condition still has to be faced of treating more effectively the symptoms (epileptic seizures) and of preventing their unfavourable evolution. So far, research has been unsuccessful involved in developing effective antiepileptic drugs (AEDs) capable of preventing the development of the pathogenic process, set in motion by different etiological factors, that leads ultimately to chronic epilepsies .[1, 2] So, a substantial need remains to develo…

Automated pre-column derivatization of amines in biological samples with dansyl chloride and with or without post-column chemiluminescence formation …

1999

On-line automation of two different liquid chromatographic procedures, a pre-column derivatization system and a pre- and post-column system, in order to generate chemiluminescence is reported. Dansyl chloride (Dns-Cl) was used as a pre-column reagent to form fluorophores and bis(2,4,6-trichlorophenyl) oxalate (TCPO) and hydrogen peroxide (H2O2) as a post-column reagent to generate chemiluminescence. This procedure is based on the employment of a primary column packed with C18 material inserted in a multi-dimensional assembly for sample clean-up and derivatization with Dns-Cl. The dansyl derivatives formed are transferred and separated in a LiChrospher 100 RP18 analytical column (125 x 4 mm …

Microbiological transformations. 30. Enantioselective hydrolysis of racemic epoxides: the synthesis of enantiopure insect juvenile hormone analogs (b…

1993

Abstract The enantioselective epoxide biohydrolysis of the racemic benzodioxole 6,7-epoxygeraniol derivative 1 has been achieved using the fungus A. niger . This new type of preparative scale bioconversion allows the synthesis of both enantiomers of Bower's compound, an analogue of insect juvenile hormone. Biological tests showed that the 6(R) enantiomer was about ten times more active than the 6(S) enantiomer against the yellow meal worm Tenebrio molitor .

Modification of halloysite lumen with dopamine derivatives as filler for antibiofilm coating

2023

Hypothesis: Development of nanocomposite coating with antibiofilm properties is of fundamental importance to efficient fight biofilm formation preventing infections in biomedical area. In this context, halloysite nanotubes (HNTs), biocompatible and low-cost clay mineral, have been efficiently used as filler for different polymeric matrices affording several nanocomposites with appealing antimicrobial properties. The modification of HNTs surfaces represents a valuable strategy to improve the utilization of the clay for biological purposes. Experiments: Herein, the covalent modification of the HNTs lumen with properly designed dopamine derivatives with different perfluoroalkyl chain length is…

Biphenyls and xanthones from the podostemaceae

1992

Abstract Investigation of the fruiting parts of Mourera fluviatilis afforded 6-desoxyjacareubin, trapezifoliaxanthone and a series of eight new biphenyl derivatives; 3,5-dimethoxybiphenyl; 2,2-dimethyl-5-methoxy-7-phenylchromene; 2,2-dimethyl-7-methoxy-5-phenylchromene; 2-(3,3-dimethylallyl)-3-hydroxy-5-methoxybiphenyl; 2,3-dihydro-6-methoxy-4-phenyl-2,3,3-trimethylcoumarone; [(2,3-dihydro-3,3-dimethyl-6-methoxy-4-phenyl)-2-coumaronyl]methanol; 2,3-dihydro-3,3-dimethyl-6-methoxy-2-oxo-4-phenylcoumarone; and a dimeric biphenyl.