A benzensulfonanilide-type cyclooxygenase-1 (COX-1)-selective inhibitor, ZXX2-77: 4-amino-4′-chloro-N-methylbenzenesulfonanilide (4a), has been reported as a novel analgesic that does not cause gastric damage. This compound has a weak analgesic effect but has potent in vitro COX-1 inhibitory ac...
In order to create novel analgesic agents without gastric disturbance, structurally simple cyclooxygenase-1 (COX-1) inhibitors with a benzenesulfonanilide skeleton were designed and synthesized. As a result, compounds 11f and 15a, which possess a p-amino group on the benzenesulfonyl moiety and p...
Vancomycin is mainly used as an antibacterial agent of last resort, but recently vancomycin-resistant bacterial strains have been emerging. Although new antimicrobials have been developed in order to overcome drug-resistant bacteria, many are structurally complex β-lactams or quinolones. In thi...
A novel series of benzenesulfonanilide derivatives of 11β-HSD1 inhibitors were identified via modification of the sulfonamide core of the arylsulfonylpiperazine lead structures. The synthesis, in vitro biological evaluation, and structure–activity relationship of these compounds are presented....
In the present study, fifteen novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one (6a-o) derivatives were designed as inhibitor of HIV-1 RT using ligand based drug design approach and in-silico evaluated for drug-likeness properties. Designed compounds were synthesize...
(Z)-2-((1H-Indazol-3-yl)methylene)-6-methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one is a potent and selective proviral integration site in moloney murine leukemia virus kinase 1 (PIM1) inhibitor with an IC50 value of 3 nM. (Z)-2-((1H-Indazol-3-yl)methylene)-6-[11C]methoxy-7-(piperazin-1-yl...
The coupling of acyl electrophiles with organometallic reagents represents a convergent route toward complex and versatile ketone products. Despite the mild conditions and high functional group tolerance, the cross-coupling of carboxylic acid derivatives, such as thioesters, and secondary organo...
This article describes the synthesis of a series of butyrophenone analogues in which the propyl chain is partially included in a cyclopentane ring. These trans-(2-aminomethyl)cyclopentyl aryl ketones are obtained by reacting (2-bromomethyl)cyclopentyl phenyl ketone or (2-bromomethyl)cyclopentyl ...
The INDO/S approach is used to study the structure/spectra relationship for some N,N′-disubstituted 1,4-diaminoanthraquinones. The calculated intensity and position of the short-wavelength absorption band depend on the molecular conformation, in agreement with the experimental data. The reflect...
Publisher SummaryThis chapter focuses on the synthesis of amino sugar derivatives by replacing р-tolylsulfonyloxy (tosyloxy) groups with hydrazine and subsequent reduction of the hydrazino compounds. Highly concentrated hydrazine (> 95%) can be obtained by distillation of ∼ 85% hydrazine hydra...
We have carried out experiments to derive a quantitative understanding of the physical vapor transport (PVT) process and to identify convective effects on the crystal growth process. The experimental growth velocity was several orders of magnitude lower than the theoretically predicted value. Th...
Ni and Pd–Ni nanoparticles were chemically deposited on Vulcan XC-72R carbon black by impregnation method using NaBH4 as a reducing agent. The prepared electrocatalysts were characterized by X-ray diffraction (XRD), transmission electron microscopy (TEM) and energy-dispersive X-ray spectroscopy...
Mercurous chloride (Hg2Cl2) exhibits an extraordinary combination of properties including transmittance from 0.35 to 20 μm, an anomalously slow sheer wave velocity (347 m/s), large birefringence and a high acousto-optic diffraction efficiency which make it an attractive candidate for a number o...
A new azo-ligand, 1,3-dimethyl-5-(p-carboxy-phenylazo)-6-aminouracil (H3L) containing 6-aminouracil (a biomolecule) and a carboxylic function (a potential linker) was synthesized. This ligand was then employed for complexation with Ni(II), resulting in the Ni(II)/Na(I) heterometallic {[NiNa2(μ-...
An efficient synthesis of novel functionalized 4H-pyrano[2,3-b]quinoline and 1,4-dihydrobenzo[b][1,8]naphthyridine derivatives via the one-pot reaction of 2-chloroquinoline-3-carbaldehydes, 6-aminouracils and dimedone or 3-methyl-1H-pyrazol-5(4H)-one was developed. The simple procedure, mild org...
A novel class of 6-indolypyridine-3-carbonitrile derivatives were synthesized and evaluated for antiproliferative activities to establish structure–activity relationship. The synthesis was carried out through one-pot multicomponent reaction of 3-acetylindole, aromatic aldehydes, ethyl cyanoacet...
In this work, design, preparation and performance of magnetic cellulose/Ag nanobiocomposite as a recyclable and highly efficient heterogeneous nanocatalyst is described. Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD) pattern, vibrating sample magnetometer (VSM) curve, f...
The corrosion inhibition effect of two nicotinonitriles namely, 2-amino-6-phenyl-4-(p-tolyl)nicotinonitriles (ATN) and 2-amino-4-(4-methoxyphenyl)-6-phenylnicotinonitrile (AMN), has been investigated for mild steel in 1 M HCl solution by using weight loss, electrochemical impedance spectroscopy ...
(Z)-5-(Arylaminomethylidene)-4-methyl-2,6-dioxo-1,2,5,6-tetrahydropyridine-3-carbonitriles were obtained by three-component condensation of 4-methyl-2,6-dioxo-1,2,5,6-tetrahydropyridine-3-carbonitrile with aromatic amines and trimethyl orthoformate in DMF. According to X-ray data, in the solid p...
A series of 2,5- and 3,5-diphenylpyridine derivatives was synthetised in high yields. A versatile chemical strategy allows the design of diphenylpyridines differently substituted with cationic or neutral side chains. The interaction of the molecules with DNA was investigated by biophysical and b...
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