Traditional structure activity relationship studies (SAR) have led to the development of numerous sialyl Lewisx analogs in the search for potential antiinflammatory agents. However, these methods do not take into account cluster or multivalent effects. Reported herein is the chemoenzymatic synth...

The type Ia group B Streptococcus (GBSIa) capsular polysaccharide was specifically degraded by partial Smith oxidation of 2,3-diol of the Glc in the backbone to fragments representing asialo core repeating units. Sialylation of these oligomers furnished GBSIa multiple repeating units. One, two a...

Novel 1,5-diaryl pyrazole derivatives viz. 5-(4-chlorophenyl)-1-(4-fluorophenyl)-1H-pyrazole-3-carboxamides (2a–e, 3, 3a–f), 2-(5-(4-chlorophenyl)-1-(4-fluorophenyl)-1H-pyrazole-3-yl)thiazoles (6a–c,7, 8, 9a–c, 10, 11) were synthesized by varying the active part (amide group) of pyrazole, ch...

A new group of hybrid nitric oxide-releasing anti-inflammatory drugs (NONO-coxibs) wherein an O2-acetoxymethyl-1-(N-ethyl-N-methylamino)diazen-1-ium-1,2-diolate (11a–c) NO-donor moiety is attached directly to the carboxylic acid group of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxyli...

Following a program searching for dual 5-HT reuptake inhibitors and α2-adrenoceptor antagonists started at Johnson & Johnson Pharmaceutical Research & Development, we now report on the synthesis of a series of 7-amino-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole derivatives, some of which pro...

A series of novel amino-carboxylic based pyrazole as protein tyrosine phosphatase 1B (PTP1B) inhibitors were designed on the basis of structure-based pharmacophore model and molecular docking. Compounds containing different hydrophobic tail (1,2-diphenyl ethanone, oxdiadizole and dibenzyl amines...

Activating mutations of REarrange during Transfection (RET) kinase frequently occur in human thyroid and lung cancers. An enormous effort has been devoted to discover potent and selective inhibitors of RET. Selective and potent inhibitors against constitutively active RET mutants are rare to dat...

Dirhodium(II) carboxylate catalysed reaction of diazocarbonyl compounds 2 in the presence of primary amides 1 results in the formation of α-acylaminoketones 3 (12 examples) by N–H insertion reaction of the intermediate rhodium carbene. The 1,4-dicarbonyl compounds 3 are readily converted into ...

The present work describes a novel approach for the annulation of an indole moiety onto the 1,3-diaryl-2-propen-1-one scaffold followed by trifluoroacetylation of the resultant indole-based chalcones to afford the corresponding 3-trifluoroacetylindole-chalcone derivatives. The parent indole-chal...

Triapine, the most prominent anticancer drug candidate from the substance class of thiosemicarbazones, was investigated in >30 clinical phase I and II studies. However, the results were rather disappointing against solid tumors, which can be explained (at least partially) due to inefficient deli...

The human topoisomerase IB inhibition and the antiproliferative activity of 3-(4-bromophenyl)-1-pyridin-2-ylprop-2-en-1-one thiosemicarbazone HPyCT4BrPh alone and its copper(II) complex [Cu(PyCT4BrPh)Cl] was investigated. [Cu(PyCT4BrPh)Cl] inhibits both the DNA cleavage and religation step of th...

Neutral bivalent copper and nickel bis(thiosemicarbazone) complexes bearing the methoxy and bromine substituents on the dialdehyde-backbone of the ligand have been synthesized. All of them have been characterized by spectroscopic methods and in two cases by X-ray crystallography. Upon formation ...

Although many N-heterocyclic thiosemicarbazone copper complexes have been proposed as potential anticancer agents, little is known about their intracellular localization in cells. In the present study, we synthesized two fluorescent N-heterocyclic thiosemicarbazone copper complexes, ([CuII(L)(Br...

In recent years, in concern for human health, a dynamic growth in the production of ethyl esters of flexeed oil was observed. However the main by-product generated in the manufacture of esters is the glycerol fraction contains raw glycerol and polyunsaturated fatty acids. The presented study was...

The disaccharide of 6-O-(2-tetradecylhexadecanoyl)muramoyl dipeptide coupled through an α-(1↔1)-α linkage, named in the title, and an analog bearing a single peptide moiety, have been synthesized from 2,2′-diazido-2,2′-dideoxy-α,α′-trehalose. The immunoadjuvant activities of the products ...

The synthesis of scandium complexes supported by two bis(trimethylsilyl)amido ligands and their reactivity to generate a variety of organometallic derivatives is reported. The monomeric scandium complex Sc{N(SiMe3)2}2(THF)Cl, 1, and the “ate” complex Sc{N(SiMe3)2}2Cl2Li(THF)3, 2, were generate...

In our previous study, we reported a series of 1-hydroxy-2-phenyl-1H-imidazole-5-carboxylic acid derivatives that presented excellent in vitro xanthine oxidase (XO) inhibitory potency. To further investigate the structure-activity relationships of these compounds, the imidazole ring was transfor...

Synthesis, physicochemical and anticonvulsant properties of new N-Mannich bases derived from 5-cyclopropyl-5-phenyl- and 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-diones have been described. Initial anticonvulsant screening was performed using intraperitoneal (ip.) maximal electroshock ...

Enantiopure N-benzyloxycarbonyl-protected and free 3-substituted homotaurines were synthesized from naturally occurring amino acids via N-benzyloxycarbonyl protection, Arndt–Eistert homologation, reduction, esterification with thioacetic acid, and oxidation with performic acid. The current meth...

Unexpected oxidation of the condensation product of 2-(diphenylphosphino)benzaldehyde and 2-aminothiophenol afforded 2-(2,3-dihydro-1,3-benzothiazol-2-yl)phenyl(diphenyl)phosphine oxide (I). The structure of the new compound was established by means of IR and 1H, 13HC and 31P NMR spectroscopy an...