Search results for "Amides"

2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action

2013

Abstract Several new benzamides 4a–q were synthesized by stirring in pyridine the acid chlorides 3a–q with the appropriate anthranilamide derivatives 2a–g. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).

Colorimetric sensing of anions by a neutral biphenyl based amide receptor

2007

A new colorimetric sensor for fluoride is described. Compound 1 shows an open structure and its behaviour is compared with that of two related closed compounds 2 and 3. In all cases, the red colour developed in the presence of fluoride can be related to deprotonation processes, however ligand 1 gives rise to a faster colour change than 2 or 3 because of its higher flexibility. Other halides as well as carboxylates have been studied and the stoichiometry and complexation constants for the corresponding ligands have been determined. Costero Nieto, Ana Maria, Ana.Costero@uv.es ; Peransi Llopis, Sergio Manuel, Sergio.Peransi@uv.es

Structure‐Activity Relationships of Benzamides and Isoindolines Designed as SARS‐CoV Protease Inhibitors Effective against SARS‐CoV‐2

2020

Abstract Inhibition of coronavirus (CoV)‐encoded papain‐like cysteine proteases (PLpro) represents an attractive strategy to treat infections by these important human pathogens. Herein we report on structure‐activity relationships (SAR) of the noncovalent active‐site directed inhibitor (R)‐5‐amino‐2‐methyl‐N‐(1‐(naphthalen‐1‐yl)ethyl) benzamide (2 b), which is known to bind into the S3 and S4 pockets of the SARS‐CoV PLpro. Moreover, we report the discovery of isoindolines as a new class of potent PLpro inhibitors. The studies also provide a deeper understanding of the binding modes of this inhibitor class. Importantly, the inhibitors were also confirmed to inhibit SARS‐CoV‐2 replication in …

An Na8 Cluster in the Structure of a Novel oxamato-bridged Na'Cu'' three-Dimensional Coordination Polymer

1999

[EN] The new heterometallic sodium(I)¿copper(II) compound Na4Cu2 (2) · 10.5 H2O (3), where H8[2] stands for N,N',N'',N'''-methanetetrayltetrakismethylenetetrakis(oxamic acid), has been synthesized and its crystal structure determined by single-crystal X-ray diffraction. The structure of 3 consists of cationic [Cu2(¿4:¿4-2)]4- dinuclear units, coordinated sodium cations, and water molecules. In the crystal, the dinuclear copper entities are joined through discrete aggregates of eight sodium atoms linked by oxamato and water bridges, leading to a three-dimensional polymeric network.

Chemistry and reactivity of dinuclear iron oxamate complexes: alkane oxidation with hydrogen peroxide catalysed by an oxo-bridged diiron(III) complex…

2004

[EN] A new dinuclear iron(III) complex with the tetradentate ligand N,N'-o-phenylenebis(oxamate) (opba) has been synthesised, and structurally, magnetically and electrochemically characterised. It possesses an unprecedented triply bridged Fe-2(mu-O)(mu-RCO2...H2O...O2CR)(2) core, whereby two N-amides from the opba ligand complete the square-pyramidal coordination sphere of the O-carboxylate rich iron site (Fe-N = 2.053 Angstrom and Fe-O = 2.015 Angstrom), The antiferromagnetic exchange interaction between the two high-spin Fe-III ions through the oxo bridge (J = -190 cm(-1); H = -JS(1)(.)S(2)) is weaker than that found in related mu-oxo singly bridged diiron(III) complexes. The lessened ant…

Direct Anodic Dehydrogenative Cross- and Homo-Coupling of Formanilides

2018

Serial versus parallel columns using isocratic elution: a comparison of multi-column approaches in mono-dimensional liquid chromatography.

2015

Abstract When a new separation problem is faced with high-performance liquid chromatography (HPLC), the analysis is addressed conventionally with a single column, trying to find out a single experimental condition aimed to resolve all compounds. However, in practice, the system selectivity may be insufficient to achieve full resolution. When a separation fails, the usual practice consists of introducing drastic changes in the chromatographic system (e.g. use of another column, solvent or pH). An alternative solution is taking benefit of the combined separation capability of two or more columns, which can be attained in multiple ways, such as diverse modalities of two-dimensional HPLC, or mo…

Calmodulin binds to p21(Cip1) and is involved in the regulation of its nuclear localization.

1999

p21(Cip1), first described as an inhibitor of cyclin-dependent kinases, has recently been shown to have a function in the formation of cyclin D-Cdk4 complexes and in their nuclear translocation. The dual behavior of p21(Cip1) may be due to its association with other proteins. Different evidence presented here indicate an in vitro and in vivo interaction of p21(Cip1) with calmodulin: 1) purified p21(Cip1) is able to bind to calmodulin-Sepharose in a Ca(2+)-dependent manner, and this binding is inhibited by the calmodulin-binding domain of calmodulin-dependent kinase II; 2) both molecules coimmunoprecipitate when extracted from cellular lysates; and 3) colocalization of calmodulin and p21(Cip…

Gold(I)-Catalyzed Intermolecular Cycloaddition of Allenamides with α,β-Unsaturated Hydrazones: Efficient Access to Highly Substituted Cyclobutanes

2014

α,β-Unsaturated N,N-dialkyl hydrazones undergo a mild [2 + 2] cycloaddition to allenamides when treated with a suitable gold catalyst. The method, which represents the first application of N,N-dialkyl hydrazones in gold catalysis, is compatible with a wide variety of substituents at the alkenyl moiety of the hydrazone component, proceeds with excellent levels of regio- and diastereoselectivity, and provides densely substituted cyclobutanes with good to excellent yields.

The phosphodiesterase 4 inhibitor roflumilast augments the Th17-promoting capability of dendritic cells by enhancing IL-23 production, and impairs th…

2016

Phosphodiesterase 4 (PDE4) inhibitors serve to prevent degradation of the intracellular second messenger cAMP, resulting in broad anti-inflammatory effects on different cell types including immune cells. Agents that elevate cAMP levels via activation of adenylate cyclase have been shown to imprint a Th17-promoting capacity in dendritic cells (DCs). Therefore, we studied the potential of therapeutically relevant PDE inhibitors to induce a pronounced Th17-skewing capacity in DCs. Here we show that mouse bone marrow-derived (BM-) DCs when treated with the PDE4 inhibitor roflumilast (ROF, trade name: Daxas) in the course of stimulation with LPS (ROF-DCs) evoked elevated IL-17 levels in cocultur…