A protocol of [3 + 3]-cycloaddition was proposed for the synthesis of 2H-1,4-thiazin-3(4H)-ones and thiomorpholine-3,5-diones from α-chlorohydroxamates and 1,4-dithiane-2,5-diol. This direct and practical method provides a novel and rapid approach for the synthesis of thiomorpholin-3-one deriva...

N-Chloroacetyl-5-bromoanthranilic acid (1), 3-[4′-(p-chlorophenyl)-thiazol-2′-yl]-2-chloromethyl-6-bromoquinazolin-4-one (2), 3-[4′-(p-chlorophenyl)-thiazol-2′-yl]-2-hydrazinomethyl-6-bromoquinazolin-4-one (3), 3-[4′-(p-chlorophenyl)-thiazol-2′-yl]-2-substitutedbenzylidene aminomethyl-6-br...

The base-induced formal [4 + 3] annulation reactions of N-(ortho-chloromethyl)aryl amides with nitrones or hydrazonoyl chlorides have been reported. When nitrones are used as the 1,3-dipole, the corresponding reaction afforded a series of 1,2,3,5-tetrahydrobenzo[e][1,2,4]oxadiazepine derivatives...

Novel bipolar benzothiazole-based derivatives with various π-electron donors were synthesized and characterized using 1H and 13C NMR and mass spectrometry; their thermal, optical and electrochemical properties were also investigated. Optoelectronic properties are reported and discussed in terms...

Three new D–π–A type compounds, each containing one benzothiazole ring as an electron acceptor and one N-ethylcarbazole group as electron donor, were synthesized and characterized by elemental analysis, NMR, MS and thermogravimetric analysis. The absorption and emission spectra of three compo...

The π-conjugated donor-acceptor stilbenoid dendrimers are successfully synthesized in high yields by either Aldol-type condensation or Wittig reaction with triphenylamine as donor and benzothiazole as acceptor. The molar extinction coefficient increases with increase in the number of the conjug...

This study was undertaken to investigate the role of the aldose reductase in the refractoriness of diabetic rats to allergic inflammation. Wistar rats were actively sensitized with a mixture of Al(OH)3 plus ovalbumin and intrapleurally challenged with ovalbumin, 14 days later. Diabetes was induc...

Vascular endothelial growth factor (VEGF) plays important roles in tumor angiogenesis, and the inhibition of its signaling pathway is considered an effective therapeutic option for the treatment of cancer. In this study, we describe the design, synthesis, and biological evaluation of 2-acylamino...

The wave functions for calculation of 13C nuclear magnetic shielding tensors of this molecule have been optimally selected using factorial design as a multivariate method. The calculating of 13C shielding constants engaged the Gaussian 03 implementation of the GIAO by using 16 different basis se...

A new chemoenzymatic method is proposed for the synthesis of enantiomerically pure 4-phenyl-1,4-dihydro-2H-isoquinolines based on the enzymatic kinetic resolution of 2-acetyl-4-phenyl-1,4-dihydro-2H-isoquinolin-3-one. For the enzymatic resolution of the racemic substrate, readily available ‘hom...

The present communication deals with the synthesis of a series of 2-acetyl-2-ethoxycarbonyl-1-[4(4′-arylazo)-phenyl]-N,N-dimethylaminophenyl aziridines. The compounds were synthesized in excellent yields (70–80%) and the structures were established on the basis of consistent IR, 1H NMR and ele...

Variable-temperature 13C NMR spectroscopy is used to investigate barrier of C-N internal rotation in compound 4- (Phenyl) acetyl morpholine, and then with simulation of band shape broadening pattern at coalescence region, rate constants of exchange were obtained for all temperatures. For simulat...

Janus kinases (JAKs) regulate various inflammatory and immune responses and are targets for the treatment of inflammatory and immune diseases. Here we report the discovery and optimization of 1H-pyrazolo[3,4-d]pyrimidin-4-amino as covalent JAK3 inhibitors that exploit a unique cysteine (Cys909) ...

Two new dinuclear copper(II) and zinc(II) complexes of an isoindol functionality based new dinucleating ligand, H3hdpa (H3hdpa = 2-({[2-hydoxyethyl]-[2-hydroxy-3-(1-oxo-1,3-dihydro-isoindol-2-yl)-propyl]-amino}-methyl)-benzoic acid) have been synthesized and characterized. In methanol, the react...

Three series of S-(1(3H)-isobenzofuranone-3-yl)isothiuronium bromides differing in substitution at the isothiuronium moiety (none, one or two methyl groups) and at the benzene ring were prepared and characterized. These salts were then treated with various bases (acetate, triethylamine, Na2CO3) ...

The parallel acylation of N-{3-[4-(3-aminopropyl)piperazin-1-yl]propyl}-7-chloroquinolin-4-amine with polymer-bound carboxylic acids opened straightforward access to novel aminoquinolines with activity against Plasmodium falciparum strains in vitro. Using this amino scaffold prepared in solution...

The reaction of 4′-substituted terpyridyl ligand of 4′-hydroxy-2,2′:6′,2″-terpyridine (tpyOH) with zinc(II) acetate resulted in the formation of [Zn(tpyO)(OCOCH3)] (1). Complex 1 forms a one-dimensional polymer via coordination through oxygen atom in which tpyO− acts as a tetra-dentate liga...

Three new d8 transitions metal complexes containing substituted-2,2′:6′,2″-terpyridine ligands of [NiII(pytpy)2]Cl2. H2O (pytpy = 4′- (4-pyridyl)-2,2′:6′,2″-terpyridine) (1), [Pt(tpyOH)Cl]+Cl−. 2H2O (2) (tpyOH = 4′-hydroxy-2,2′:6′,2″-terpyridine) and [Pt(tpySH)Cl]+Cl−.2H2O (3) (tpySH ...

Herein, we report the design and synthesis of three novel binuclear platinum(II) complexes, [Pt(tpbtpy)Cl][Pt(DMSO)Cl3] (tpbtpy-Pt), [Pt(dthbtpy)Cl][Pt(DMSO)Cl3]⋅CH3OH (dthbtpy-Pt), and [Pt(qlbtpy)Cl][Pt(DMSO)Cl3]⋅CH3OH (qlbtpy-Pt) with 4′-(3-thiophenecarboxaldehyde)-2,2′:6′,2″-terpyridine (...

The key intermediates for the Kröhnke methodology for the synthesis of oligopyridines, 4-functionalised-2,6-diacetylpyridines (4-substituent=Cl, OEt or benzyloxy) have been synthesised. 4-Ethoxy-2,6-diacetylpyridine was reacted to give novel 4′-ethoxy-2,2′:6′,2″-terpyridines which possess su...