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Leht 1 alates 22 tulemused
The crystal structure of the 1:1 inclusion complex of beta-cyclodextrin with benzamide.
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The 1:1 inclusion complex of beta-cyclodextrin and benzamide was prepared and characterized by single crystal X-ray diffraction, PXRD, TGA, and IR. This complex crystallizes in the monoclinic P2(1) space group with unit cell constants a=15.4244(16), b=10.1574(11), c=20.557(2)A, beta=110.074(2)
A bis(triazole)benzamide receptor for the complexation of halide anions and neutral carboxylic acid guests. Guest-controlled topicity and self-assembly.
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Bis(triazole)benzamide 1 has been readily synthesized by means of Cu-catalyzed 1,3-dipolar cycloaddition and its ability to bind halide anions and neutral gallic acid derivative 12GA has been theoretically and experimentally investigated. The cavity defined by the N-H amide group and the vicinal
The filaricidal activity of some derivatives of N-[2-(4-thiazolyl)benzimidazol-5-yl]benzamide against Brugia pahangi adults.
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A series of analogues of N-[2-(4-thiazolyl)benzamidazol-5-yl]benzamide with halogen substituents on the benzamide ring was tested for activity against adult Brugia pahangi in the peritoneal cavities of jirds. None of the chloro, bromo or iodo analogues was active at 5 x 100 mg/kg by subcutaneous
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
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A series of benzamide derivatives including two scaffolds were designed and synthesized as potential histone deacetylase inhibitors. Most of synthesized compounds showed moderate enzymatic potency at the same order of magnitude, and compound 12b possessed better potency to the positive control (3.8
Target Identification and Mechanism of Action of Picolinamide and Benzamide Chemotypes with Antifungal Properties.
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Invasive fungal infections are accompanied by high mortality rates that range up to 90%. At present, only three different compound classes are available for use in the clinic, and these often suffer from low bioavailability, toxicity, and drug resistance. These issues emphasize an urgent need for
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
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Significant effort is being made to understand the role of HDAC isotypes in human cancer and to develop antitumor agents with better therapeutic windows. A part of this endeavor was the exploration of the 14 A internal cavity adjacent to the enzyme catalytic site, which led to the design and
Development of Helical Aromatic Amide Foldamers with a Diphenylacetylene Backbone.
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We designed and synthesized aromatic polyamides with a diphenylacetylene backbone, α-DPA and β-DPA, bearing (S)-α- and (S)-β-methyl-substituted triethyleneglycol (TEG) side chains, respectively, and examined their conformations in solution. Both polymers exhibit strong,
Identification of novel Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitors using computational approaches.
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Nicotinamide Phosphoribosyltransferase (NAMPT) is a rate-limiting enzyme in the biosynthesis of NAD. Cancer cells have elevated poly [ADP-Ribose] polymerase 1 (PARP) activity as well as the immense necessity of ATP: thereby consuming NAD at a higher rate than normal tissues. The perturbation of
Unique gradual and sustained vasodilator response to substance P in the rabbit knee joint.
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The effects of substance P on blood flow, plasma extravasation, and knee joint sizes in the rabbit were investigated. Topical bolus application of substance P (1 nmol) onto the exposed rabbit knee joint capsule increased its blood flow from 15 min onwards and reached a peak of 46% at 90 min compared
Supramolecular assembly of self-labeled amphicalixarenes.
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The synthesis and precise supramolecular organization of new amphicalixarene 4 bearing four rodlike aligned fluorescent terephthalic benzamide moieties in the upper rim is reported. The aggregation of 4 was monitored by a combination of fluorescence, conductometry, and cryo-TEM measurements at
Overlapping binding sites of structurally different antiarrhythmics flecainide and propafenone in the subunit interface of potassium channel Kv2.1.
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Kv2.1 channels, which are expressed in brain, heart, pancreas, and other organs and tissues, are important targets for drug design. Flecainide and propafenone are known to block Kv2.1 channels more potently than other Kv channels. Here, we sought to explore structural determinants of this
Supramolecular photochirogenesis. 2. Enantiodifferentiating photoisomerization of cyclooctene included and sensitized by 6-O-modified cyclodextrins
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Supramolecular enantiodifferentiating photoisomerization of (Z)-cyclooctene (1Z) to the chiral (E)-isomer (1E) via inclusion and sensitization by modified alpha-, beta-, and/or gamma-cyclodextrin derivatives, possessing benzoate (2a, 3a, 4a), isomeric phthalates (3b-d), and tethered benzamide (3e)
Synthesis and characterization of a tripodal amide ligand and its binding with anions of different dimensionality.
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Synthesis and crystal structure of a tren-based amide, L(1), N,N',N''-tris[(2-amino-ethyl)-3-nitro-benzamide] is reported. The crystallographic results show intramolecular hydrogen bonding and aromatic pi...pi stacking among tripodal arms which prevent opening of the receptor cavity. Intermolecular
[Novel Helical Foldamers Based on the Conformational Properties of Aromatic Amides].
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In this review, we focus on our recent work on the development of novel helical foldamers based on the cis conformational properties of aromatic amide bonds. First, we describe the conformational properties of N-alkylated pyrroleamides and their oligomers. The conformation of the amide bond on the
The cyclic "silver-diphos" motif [Ag2(mu-diphosphine)2]2+ as a synthon for building up larger structures.
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The dinuclear, cyclic structural motif [Ag2(diphosphine)2](2+), here termed the "silver-diphos" motif, previously observed in many diphosphine-silver complexes, has been investigated as a synthon for building up larger structures such as coordination cages and polymers. A series of ligands
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