The over-expression of aminopeptidase N on diverse malignant cells is associated with the tumor angiogenesis and metastasis. In this report, one new series of leucine ureido derivatives containing the triazole moiety was designed, synthesized and evaluated as APN inhibitors. Among them, compound...

Two new total syntheses of 1-methyl-1,2,3,4-dihydronaphtho[1,2-f]isoquinolines are based on the construction of their phenanthrene ring system by photochemically induced cyclization of N-{2-[(E)-2-phenyl-1-ethenyl]phenylethyl}acetamides or 1-methyl-5-[(E)-2-phenyl-1-ethenyl]-1,2,3,4-tetrahydrois...

As a part of our drug discovery program, we identified an alkaloidal amide i.e. Aegeline (V) isolated from the leaves of Aegle marmelos as a dual acting agent (antihyperlipidemic and antihyperglycemic). In continuation of this program, we synthesized new N-acyl-1-amino-2-alcohols (N-acrylated-1-...

The base-promoted aromatic [3,3] sigmatropic rearrangement of N-acyl-O-arylhydroxylamines giving α-(2-hydroxyphenyl)amides was successfully demonstrated. The substrates were prepared from N-substituted hydroxylamines by N-acylation followed by copper(I)-mediated O-arylation with boronic acids. ...

The inhibitory activity (IC50) toward matrix metalloproteinases (MMP-1, MMP-2, MMP-3, MMP-9, and MMP-13) of N-hydroxy-2-[(phenylsulfonyl)amino]acetamide derivatives (HPSAAs) has been successfully modeled using 2D autocorrelation descriptors. The relevant molecular descriptors were selected by li...

2,2,2-Trichloro-N-[(trimethylsilyl)methyl]acetamide and 2,2,2-trimethyl-N-[(trimethylsilyl)-methyl]acetamide were prepared by reaction of N-[(trimethylsilyl)methyl]amine with acid chlorides of the corresponding acids. The crystal structure of 2,2,2-trichloro-N-[(trimethylsilyl)methyl]acetamide w...

A series of bis-carbamate-based low-molecular-weight organogelators were synthesized, and their structure–property relationships with respect to their gelation abilities in organic solvents were investigated. The self-aggregation behavior of the thermoreversible organogels was investigated by F...

Four new 3,5-disubstituted pyrazoles HpzR2 containing long-chain 4-n-alkyloxyphenyl substituents [R=C6H4OCnH2n+1; n=4 (1), 6 (2), 12 (5), 14 (6)] have been prepared and characterised. All of them showed mesomorphic behaviour, the stability and the range of the mesophases increasing with the leng...

We have synthesized a new series of quinoline tripartite hybrids from chloroquine, ethambutol, and isoxyl drugs, using a short synthetic route. Compounds 1–8 were tested in vitro against five protozoa (Giardia intestinalis, Trichomonas vaginalis, Entamoeba histolytica, Leishmania mexicana and T...

BrF3 reacts with monosubstituted phenyltrifluorosilanes X-C6H4SiF3 (X = H, p-Me, p-MeO, m-F, p-F, m-CF3, p-CF3) in equimolar reactions (CH2Cl2/MeCN solution, optimised reaction temperature) with three different patterns of products. Electron-rich aryl groups (X = H, p-Me, p-MeO) are only fluorin...

The ion/molecule reactions of phenyltrifluorosilane with F−, CH3O− and OH− and the thermochemical properties of the resulting ions were investigated by using a flowing afterglow—triple quadrupole mass spectrometer. The silane reacts with fluoride and methoxide ions by addition, whereas the reac...

To explain the formation of protein nitration marker, 3 nitrotyrosine (3NT), in food products was the basis for the present study. For the accurate detection as protein nitration marker of 3NT in food products, i) a new method was improved, which is optimized parameters affected the formation of...

DJ-1 is one of the important genes found in Parkinson's disease (PD). Studies have shown that the DJ-1 protein levels are elevated in the cerebrospinal fluid (CSF) and plasma of sporadic PD patients, and the DJ-1 protein levels in the CSF and plasma may serve as biomarkers of PD. However, J...

Novel bioactive heterocycles containing a 3,4,5-trimethoxyphenyl fragment as antiproliferative agents by targeting tubulin were synthesized and their preliminary structure activity relationships (SARs) were explored. Among all these chemical agents, 2-(Benzo[d]oxazol-2-ylthio)-N-(4-methoxybenzyl...

Mitogenicity is the ability of the natural or synthetic compounds to induce cell division or proliferation. A series of salicylic acid derivatives containing isoxazoline moiety (8a-j) were synthesized and their immunopharmacological activities targeting lymphocyte proliferation and angiogenesis ...

A novel acidic ionic liquid (AIL), 3-(2-carboxybenzoyl)-1-methyl-1H-imidazol-3-ium chloride {[Cbmim]Cl}, was synthesized and used as an efficient and green catalyst for the Biginelli reaction under solvent-free conditions. The present study aims to develop an improved synthesis procedure, based ...

The reaction of CuCl2·2H2O with 1-(2-carboxybenzoyl)thiosemicarbazide (H3L) and imidazole (HIm) in NaOH gave a CuII complex, which was crystallized from pyridine (Py) to give complex 1, [Cu3L2(Py)6(HIm)](H2O)2. The complex molecule contains a linear Cu3 array in which the central copper atom at...

This paper describes the application of 3-(4-carboxybenzoyl)quinoline-2-carboxaldehyde (CBQCA), a sensitive fluorogenic reagent for detection of amines, to the assay of proteins in solution. The sensitivity and dynamic range of CBQCA in the determination of protein concentration is modulated by ...

Detection of amino acids by laser-induced fluorescence capillary electrophoresis can be achieved by using a fluorogenic reagent, 3-(p-carboxybenzoyl)quinoline-2-carboxaldehyde (CBQ). This reagent does not fluoresce unless it has reacted with a primary amine to form an isoindole derivative. Using...

A RP-LC-FL detection method has been developed to identify and quantitate four amino acid neurotransmitters including glutamic acid, glycine, taurine and γ-aminobutyric acid in rat and mouse spinal cord tissue. 3-(4-carboxybenzoyl)-2-quinolinecarboxaldehyde (CBQCA) was employed for the derivati...