N-Formyl peptide receptors (FPRs: FPR1, FPR2, and FPR3) are G protein-coupled receptors that play key roles in modulating immune cells. FPRs represent potentially important therapeutic targets for the development of drugs that could enhance endogenous anti-inflammation systems associated with va...
A new series of 2-substituted mercapto-4(3H)-quinazolinone 1–26 were synthesized and assessed for in vivo anti-inflammatory and analgesic activities and in vitro inhibition of cyclooxygenase COX-1/COX-2.A new series of 2-substituted mercapto-4(3H)-quinazolinone 1–26 were synthesized and assess...
A series of 2-anilinopyridine dimers have been synthesized and evaluated for their anticancer potential. Most of the compounds have showed significant growth inhibition of the cell lines tested and compound 4d was most effective amongst the series displaying a GI50 of 0.99 μM specifically again...
Cobalt(II), nickel(II), copper(II), zinc(II) and hafnium(IV) complexes of furan-2-carbaldehyde 4-methoxy-N-anilinoacetohydrazone were synthesized and characterized by elemental and thermal (TG and DTA) analyses, IR, UV–vis and 1H NMR spectra as well as magnetic moment and molar conductivity. Mo...
One-step antisolvent deposition has been considered as one of the most feasible methods to obtain high-performance perovskite solar cells (PSCs). However, most of the reported high-performance PSCs are based on the toxic anti-solvents, which is a major issue for the potential commercialization o...
The preparation of p-[ethyl-(2-chloroethyl)amino]oxanilic acid, 5-[ethyl-(2-chloroethyl)amino]salicylic acid and 5-(di-2-chloroethylamino)salicylic acid is described. The results of a preliminary screening of these new compounds against the transplanted Walker rat carinoma are reported.
The preparation of (S)-3-methylamino-3-[(R)-pyrrolidin-3-yl]propanenitrile (1), a key fragment of fluoroquinolone antibiotic PF-00951966 and others was achieved by N-methylative aziridine ring opening, addition of methyl group at the ring nitrogen, and ring-opening via a cyanide nucleophile in a...
β-Methylamino-l-alanine (BMAA) is a neurotoxic amino acid that can be produced by cyanobacteria in aqueous environments. To analyze this compound by gas chromatography/mass spectrometry (GC/MS), BMAA must be derivatized to a nonpolar, volatile compound. This can be accomplished by reacting BMAA...
A series of novel 2-benzylthio-4-chloro-5-(5-substituted 1,3,4-oxadiazol-2-yl)benzenesulfonamides (4–27) have been synthesized as potential anticancer agents. MTT assay was carried out to determine the cytotoxic activity against three human cancer cell lines: colon cancer HCT-116, breast cancer...
A series of benzenesulfonamide derivatives were synthesized and evaluated for their anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferative and tubulin polymerization. Compound BA-3b proved to be the most potent...
Ureido-substituted benzenesulfonamides (USBs) show great promise as selective and potent inhibitors for human carbonic anhydrase hCA IX and XII, with one such compound (SLC-0111/U-F) currently in clinical trials (clinical trials.gov, NCT02215850). In this study, the crystal structures of both hC...
A film of benzenesulfonamide azo dye has been prepared by spray pyrolysis method onto BK7 glass substrate with average thickness of 2.7 μm. This azo dye was derived from sulfamethoxazole and chromotropic acid by the Fox method. The optical constants (refractive index, n, extinction coefficient,...
Benzotriazoles, benzothiazoles and benzenesulfonamides are high-volume production chemicals widely used in industry and households every day. They are highly soluble in water and some resist biodegradation and/or have toxic effects. They have already been classified as emerging organic pollutant...
Herein, we reported three polyzwitterions: binary one (PAAS) synthesized with acrylamide (AM) and 2-((3-methacrylamidopropyl)dimethylammonio)ethyl sulfite (MAPES), and two ternary (PABA, PADA) with AM, MAPES and benzene sulfonamides. The polyzwitterions were successful synthesized and proved by ...
Two series of benzenesulfonamides bearing methyl groups at ortho/ortho or meta/ortho positions and a pyrrolidinone moiety at para position were synthesized and tested as inhibitors of the twelve catalytically active human carbonic anhydrase (CA) isoforms. Observed binding affinities were determi...
N,N-Dichloro-p-toluenesulfonamide (TsNCl2) was found to be an efficient nitrogen source for the aziridination of unfunctionalized alkenes using palladium catalysts. Among the palladium salts, palladium acetate was the most effective catalyst for this reaction. A variety of alkenes were reacted a...
A novel ultraviolet spectrophotometric method for the assay of microgram amounts (1–80 μg/ml) of CAT and CAB in aqueous solution has been developed. The method is highly sensitive, simple, and rapid within the limits of the experimental conditions described. The present method is also applicab...
Cathodic reduction of several secondary and tertiary p-toluenesulfonamides and gem-N-disulfonamides were investigated by cyclic voltammetry and controlled potential electrolysis at mercury electrode in aprotic and protic dmf. In the cleavage of tertiary p-toluenesulfonamides two Faradays per mol...
The alkylammonium salt of chloramine-T has been used as aminating agent of olefins in the presence of M(TPP)Cl (M = Fe, Mn; TPP = tetraphenylporphyrin) as catalyst. Main products were the corresponding allylamine, the aziridine, the α-chloro-amine derived by attack of chloride ion on the less s...
Hg cathode-free electrochemical detosylation of N,N-disubstituted p-toluenesulfonamides was successfully carried out by a constant current electrolysis using an undivided cell equipped with a platinum cathode and a magnesium anode in the presence of an arene mediator. The deprotection proceeded ...
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