Bis(methylsulfanyl) derivatives of iron(II) bis(dicarbollide) [8,8′-(MeS)2-3,3′-Fe(1,2-C2B9H10)2]2- (42−), [4,4′-(MeS)2-3,3′-Fe(1,2-C2B9H10)2]2- (52−), and [4,7′-(MeS)2-3,3′-Fe(1,2-C2B9H10)2]2- (62−) were prepared by the treatment of the corresponding dimethylsulfonium derivatives 1–3 wit...

In present study, a series of novel containing trifluoromethyl 4-(2-pyrimidinylamino)benzamide derivatives were designed by the fluorine scan strategy. Their Hh signaling inhibitory activities were evaluated by Gli-luciferase reporter method. The comprehensive SAR was discussed and several deriv...

A convenient and user-friendly method to yield benzamides from primary and secondary amines and various benzylic alcohols in the presence of a cheap iron salt (FeCl2·4H2O) and tert-butylhydroperoxide (70% in water) as a stoichiometric oxidant is described. Control experiments indicated that thi...

A series of novel hedgehog signaling pathway inhibitors have been designed and synthesized based on our previously reported scaffold of 4-(2-pyrimidinylamino)benzamide. The Hh signaling pathway inhibitory activities were evaluated by Gli-luciferase reporter method and most compounds showed more ...

Previously it was reported that combining antibiotics with L-97-1, an adenosine A1 receptor antagonist, significantly improves survival and blocks acute lung injury induced by Yersinia pestis CO 99 in a rat model of pneumonic plague. In the current studies using a conscious rat model of cecal li...

L-NAME-induced hypertension is commonly used to study endothelial dysfunction and related vascular effects. It has been reported that genetic deletion of A1 adenosine receptor (AR) reduces blood pressure (BP) increases in mice and thus, suggesting the involvement of A1AR. Thus, we sought to dete...

As a result of the various N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives with a hydroxy moiety synthesized in an effort to discover novel glycogen phosphorylase (GP) inhibitors, 5-chloro-N-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide (5b) was found to have poten...

A series of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives were prepared and evaluated as inhibitors of human liver glycogen phosphorylase a (hLGPa). One compound, 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide (2f), inhibited hLGPa with an IC50 of 0.90 μM. The pyridine ...

The optical properties (photophysics and imaging) of Indian yellow were investigated both in solid state and in aqueous solution and correlated with its chemical composition. The analyses were corroborated by a theoretical study carried out on the different xanthone derivatives that comprise the...

The 1-(4-Fluorobenzoyl)-3-(isomeric fluorophenyl)thioureas (1–3) were prepared by the reaction of 4-fluorobenzoyl isothiocyanate produced in situ with isomeric fluoroanilines in dry acetonitrile in good yields. The novel compounds were characterized by multinuclear (1H and 13C) NMR, elemental a...

An asymmetric conjugate addition reaction between a chiral α,β-unsaturated amido ester and ethyl-N-methylmalonamide has been used as a key step in the synthesis of (3S,4R)-(−)-trans-4-(4′-fluorophenyl)-3-hydroxymethyl-N-methylpiperidine, a key intermediate for (−)-paroxetine.

In the present study, novel 2-cyclopropyl-3-ethynyl-4-(4-fluorophenyl) quinolines (4a-l) were recognized and evaluated as G-Protein Coupled Receptor (GPCR) ligands through molecular evaluations. Thrombin mediates adhesion of mast cell, a type of cell abundantly found in connective tissue and rel...

A library of iminolactones was prepared by esterification of several 2-hydroxyketones with a number of N-protected d- and l-α-amino acids. Some of the hydroxyketones were of terpenoid origin while others were obtained via synthesis. After N-deprotection of the intermediate esters, the free amin...

A series of novel 4-hydroxybenzaldehyde derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were investigated. Most of target compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). ...

This study focuses on analysis of local structural arrangements of ferric and ferrous iron in binary alkali-silicate networks, and the effect of changing Fe2+/Fe3+ ratio on the glass structure, investigated by Raman spectroscopy. Three alkali trisilicate glasses, Li2Si3O7, Na2Si3O7 and K2Si3O7, ...

A study of the dielectric permittivity and loss of sodium trisilicate glass over a frequency range 12 Hz to 100 kHz and temperature range 77 K to 435 K shows that its conductivity increases non-linearly with frequency and does not merge into a single line of the log conductivity-log frequency pl...

The diffusivity of sulphur in nominal 10 Na2O–16 CaO–74 SiO2 (NCS) and 26 Na2O–74 SiO2 (NS3) melts was investigated in the temperature range 1273–1473 K using the 35S radioactive isotope in a sandwich setup. Samples were sealed in platinum capsules and run with vertical alignment at 100 MPa ...

A novel and efficient one pot synthesis was developed for 2,6-substituted-benzo[d]thiazole analogues 4a–k and 2,4-substituted-benzo[d]thiazole analogues 4l–p via three component condensation reaction of substituted arylaldehyde, 2-amino-6-halo/4-methyl-benzo[d]thiazole and 2-naphthol or 6-hydr...

A novel dye, 2-{(E)-[(2-hydroxy-5-methylphenyl)imino]methyl}-4-[(E)-phenyldiazenyl]phenol dye was synthesized by the condensation reaction of 2-hydroxy-5-[(E)-phenyldiazenyl]benzaldehyde with 2-amino-4-methylphenol in methanol. The title dye was characterized by its melting point, elemental anal...

The solubility of 2,4-dihydro-5-methyl-2-(4-methylphenyl)-3H-pyrazol-3-one in twelve organic solvents including methanol, ethanol, n-propanol, isopropanol, ethylbenzene, toluene, n-butanol, acetonitrile, ethyl acetate, 1,4-dioxane, cyclohexane and isopentanol were determined experimentally by us...