BackgoundGout is an inflammatory arthritis characterized by abrupt self-limiting attacks of inflammation caused by precipitation of monosodium urate crystals (MSU) in the joint. Both anti-hyperuricemia and anti-inflammation could be gout therapeutic strategies, whereas ideal drugs for gout treat...

The intent of this study was to examine human and bovine lactoferrin fragments including lactoferrin (1-11), lactoferricin and lactoferrampin, all of which did not demonstrate hemolytic activity toward rabbit erythrocytes at 1 mM concentration, for possible inhibitory effects on the activities o...

Viral infectivity factor (Vif) is protective against APOBEC3G (A3G)-mediated viral cDNA hypermutations, and development of molecules that inhibit Vif mediated A3G degradation is a novel strategy for blocking HIV-1 replication. Through optimizations of the central ring of N-(2-methoxyphenyl)-2-((...

A thermally responsive nanogel is used to create stationary zones of enzyme and lectin in a separation capillary. Once patterned in the capillary, analyte is driven through the zone, where it is converted to a specific product if an enzyme is used or captured if a lectin is used. These stationar...

It is well known that Wnt5a activation plays a pivotal role in brain injury and β-arrestin2 induces c-Jun N-terminal kinase (JNK3) activation is involved in neuronal cell death. Nonetheless, the relationship between Wnt5a and JNK3 remains unexplored during cerebral ischemia/reperfusion (I/R). I...

A novel series of 5-bromo-pyrimidine derivatives (5a-l, 6a-h, 9a-m and 10a-d) were synthesized through multi step reactions starting from 5-bromo-2,4-dichloro pyrimidine. The newly synthesized compounds were characterized using elemental analysis and spectral data (IR, 1H NMR, 13C NMR and LC-MS)...

A total of 29 novel compounds bearing N1-(2-aryl-1, 3-thiazolidin-4-one)-N3-aryl ureas were designed, synthesized and evaluated for their biological activities. The structure-activity relationships (SARs) and binding modes of this series of compounds were clarified together. Compound 29b was ide...

Two series of novel aryl-acrylic derivatives were designed, synthesized, and screened in enzymatic and cellular inhibitory activities. All compounds showed moderate to significant potency. The SAR analyses indicated that the semicarbazone linker is better than the 1,2,3-triazole linker. Among se...

Treatment of trifluoroacetaldehyde ethyl hemiacetal with enamines, derived from acetophenone derivatives, at room temperature gave (E)-1,1,1-trifluoro-4-morpholino-4-aryl-but-3-en-2-ols, which are intermediates for preparation of the β-trifluoromethylated aldol products, 4,4,4-trifluoro-3-hydro...

The title reaction gives, depending on conditions, either a substituted tetraenic ω-dimethylaminodinitrile or a substituted 1,1,3,11,13,13-hexacyanotrideca-1,3,5,7,9,11-hexaenide salt; a series of new cation–anionic polymethyne dyes have been obtained from the latter.

The reaction of alkylidenemalononitriles with β-dimethylaminoacrolein aminal unexpectedly results in (3-dimethylaminopropen-1-ylidene)malononitrile, whereas the reaction of 1-dimethylamino-1,3,3-trimethoxypropane gives unknown ω,ω-bis(3-dimethylaminopropen-2-ylidene)alkylidenemalononitriles.

The development of a practical and efficient synthesis of a novel PPAR α/γ dual agonist, (S)-2-(((3-fluoro-4-methylphenoxy)carbonyl)(1-(4-((5-methyl-2-phenyloxazol-4-yl)methoxy)phenyl)ethyl) amino)acetic acid (1), is described. Development of a stereoselective synthesis of the (S)-4-(1-aminoet...

The use of 2-chloro-4-nitrophenyl maltotrioside (CNP-G3) as substrate to measure amylase (EC 3.2.1.1) activity in serum directly without the use of auxiliary enzymes was evaluated at two centres. The method was precise (within-run C.V.

4-Chloro-N-(2-(2-nitrophenyl)acetoxy)-N-phenylbenzamide was synthesized and characterized by 1H NMR, 13C NMR, MS, IR and X-ray diffraction methods. The structure–property relationship and the antitumor activity based on electrochemical measurements, density functional theory calculations (DFT) ...

New monomethine dyes have been prepared by a simple and highly efficient method in acetic anhydride, in which the common pyridine-2,6-dione moiety and thiophene derivatives occupy each side of the methine unit. Among them, the ternary monomethine-azo dyes were first obtained by the particularly ...

Cu nanoparticles were prepared in successive stages: preparation of the Fe3O4 magnetic nanoparticles (Fe3O4 MNPs), coating of the Fe3O4 MNPs with tetraethyl orthosilicate (Fe3O4@SiO2), functionalization of Fe3O4@SiO2 with 3-chloropropyltrimethoxysilane (CPTMS) and 4-amino-1,2,4-triazole (AT) lig...

3-Aminopropionic acids (β-amino acids) are biologically active compounds of interest in medicinal and pharmaceutical chemistry. Twenty-one 3-amino-3-arylpropionic acids were synthesized via a facile one-pot synthesis. In addition, a series of mechanistic studies have been performed to optimize ...

Eight derivatives of N-(3-chloro-4-fluorophenyl)-2-(5-((3-(4-hydroxy-2, 2-dimethyl l-2,3-dihydrobenzofuran-5-yl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) acetamide were synthesized by reacting pyrazole having substitutions at 1 and 3 positions (phenyl and benzofuran) w...

Preparation of sulfoximide derivatives of monocyclic thiophenes is reported. Treatment of 2,4-di-tert-butylthiophene 1-oxide (4) with N-[(p-toluenesulfonyl)imino]-phenyliodinane (TsN=IPh) in the presence of Cu(MeCN)4PF6 in MeCN at room temperature provided 2,4-di-tert-butyl-1-[(p-toluenesulfonyl...

1-Cyclohexyl-3-tosylurea (HL) and its two complexes, ML2·2H2O [MNi(1), and Cd(2)], have been synthesized and characterized on the basis of elemental analyses, molar conductivities, IR spectra and thermal analyses. In addition, the DNA-binding properties of the ligand and the two complexes have ...