Search results for "Derivative"

DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL HETEROCYCLIC DERIVATIVES AS MODULATORS OF B-DNA AND G-QUADRUPLEXES DNA FUNCTIONS

Computational Studies on BaCeO3 and BaZrO3 Derivatives.

2011

Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives

2022

γ-Aminobutyric acid (GABA) represents one of the most prolific structural units widely used in the design of modern pharmaceuticals. For example, β-substituted GABA derivatives are found in numerous neurological drugs, such as baclofen, phenibut, tolibut, pregabalin, phenylpiracetam, brivaracetam, and rolipram, to mention just a few. In this review, we critically discuss the literature data reported on the preparation of substituted GABA derivatives using the Michael addition reaction as a key synthetic transformation. Special attention is paid to asymmetric methods featuring synthetically useful stereochemical outcomes and operational simplicity. This research was funded by the National Na…

Effect of linker distribution in the photocatalytic activity of multivariate mesoporous crystals

2021

The use of Metal-Organic Frameworks as crystalline matrices for the synthesis of multiple component or multivariate solids by the combination of different linkers into a single material has emerged as a versatile route to tailor the properties of single-component phases or even access new functions. This approach is particularly relevant for Zr6-MOFs due to the synthetic flexibility of this inorganic node. However, the majority of materials are isolated as polycrystalline solids, which are not ideal to decipher the spatial arrangement of parent and exchanged linkers for the formation of homogeneous structures or heterogeneous domains across the solid. Here we use high-throughput methodologi…

Essays on Risk Disclosure: Evidence from the Banking Industry

2021

Influence of side chain characteristics on the aggregation-induced emission (AIE) properties of tetrasubstituted tetraphenylethylene (TPE)

2017

[EN] Five new tetraphenylethylene (TPE) derivatives were synthesised and their aggregation-induced emission (AIE) was evaluated in mixtures of THF/water and MeOH/water. The influence of regiochemistry and length of the chains in the substituents on emissive properties was studied.

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].