Kifunensine is an alkaloid that is produced by the actinomycete Kitasatosporia kifunense and resembles the cyclic oxamide derivative of 1-aminodeoxymannojirimycin in structure. We previously showed that this compound was a potent inhibitor of the purified glycoprotein processing enzyme, mannosid...

An efficient and practical synthesis of kifunensine thioanalogs 1a–c was reported. The bicyclic azasugars fused thiazolidin-4-one 4a–c as key intermediates were first synthesized in good yields of 74–80% via one-pot tandem Staudinger/aza-Wittig/cyclization by using the pivotal azidosugars 3a ...

New series of 5-fluoro-1H-indole-2,3-dione-3-thiosemicarbazones 2a–k and 5-fluoro-1-morpholino/piperidinomethyl-1H-indole-2,3-dione-3-thiosemicarbazones 3a–r were synthesized. The structures of the synthesized compounds were confirmed by spectral data, elemental and single crystal X-ray diffra...

Two novel fluorinated diimide-diacid monomers, [2,2′-(4,4′-(4′-chloro-3′-(trifluoromethyl)biphenyl-2,5-diyl)bis(oxy)bis(3-(trifluoromethyl)-4,1-phenylene))bis(1,3-dioxoisoindoline-5-carboxylic acid)] (III) and [2,2′-(4,4′-(3′,5′-bis(trifluoromethyl)biphenyl-2,5-diyl)bis(oxy)bis(3-(triflu...

The optimized molecular structure, vibrational frequencies, corresponding vibrational assignments of 5-chloro-2-((4-chlorophenoxy)methyl)benzimidazole have been investigated experimentally and theoretically using Gaussian09 software package. The energy and oscillator strength calculated by time ...

A new anthelmintic, 3, 5-diiodo-3’-chloro-4’-(p-chlorophenoxy) salicylanilide, or rafoxanide, has been found highly effective in the treatment of Haemonchus contortus infections in sheep. The compound, given as a drench at 5 or 10 mg./kg., was highly effective when administered 8 days after ex...

Four new crystal structures of sulfur and selenium analogues of 2[1H]-pyrimidinone derivatives were determined with the use of X-ray diffraction method. The molecular geometry and intermolecular interactions of the investigated molecules were analyzed in order to find the structural features and...

Two new Pt(II) and Ru(II) complexes, [Pt(BFCY)Cl2] (1) and [RuCl2(BMCY)(DMSO)] (2) with 3-(1H-benzoimidazol-2-yl)-8-fluoro-chromen-2-ylideneamine (BFCY) and 3-(1H-benzoimidazol-2-yl)-8-methyl-chromen-2-ylideneamine (BMCY), were synthesized. The BFCY Pt(II) complex 1 adopted an approximately four...

We report here that human Ntera-2/D1 (NT-2) cells, an undifferentiated committed neuronal progenitor cell line, endogenously express a functional P2Y1 receptor, while other P2Y subtypes, except perhaps P2Y4, are not functionally expressed. Quantitative RT-PCR analysis showed that NT-2 cells abun...

Two mutations of the rat serotonin 5-HT2A receptor were made, expressed and examined for their ability to bind and be stimulated by certain tryptamines as well as their ability to bind antagonists. Mutation of Ser207 to an Ala (S207A) resulted in no substantial changes in binding of either 5-HT2...

Previous studies indicated that selected ergolines and tryptamines showed species differences for affinity to the antagonist-labeled 5-HT2 receptor. The present study examined these same compounds for affinity at the agonist-labeled 5-HT2 receptor in rat and squirrel monkey cortical homogenates ...

Proline potassium salt was successfully firstly used to catalyze the Friedlander annulation toward the synthesis of 4-trifluoromethyl-substituted quinolines from the substituted 2-trifluoroacetyl anilines and variety carbonyl compounds under mild conditions in good to excellent yields. This cata...

Various chlorodifluoromethyl ketones react readily with dialkyl or diaryl phosphites in the presence of triethylamine at the reflux temperature of tetrahydrofuran to give the corresponding dialkyl or diaryl 1-substituted-2,2-difluoroethenyl phosphates in good yields, whereas the similar reaction...

Eleven dihydroxy-2-(1-hydroxy-4-methylpent-3-enyl)naphthalene derivatives as anticancer agents through regulating cell autophagy were designed and synthesized. The anticancer activity results indicated that most compounds manifested obvious un-toxic effect on GES-1 and L-02 with IC50 from 0.58 t...

N-Protected and unprotected 2-azetidinones, protolytically activated by superacidic trifluoromethanesulfonic acid, react with aromatic compounds to give β-amino aromatic ketones in good to excellent yields (65–98%). Non-benzenoid aromatics (pyrrole and ferrocene) produced good yield (64–89%) ...

Restricted rotation about the naphthalenylcarbonyl bonds in the title compounds resulted in mixtures of cis and trans rotamers, the equilibrium and the rotational barriers depending on the substituents. For 2,7-dimethyl-1,8-di-(p-toluoyl)-naphthalene (1) ΔH° = 3.66 ± 0.14 kJ mol−1, ΔS° = ...

3-Chloropropyltrichlorogermane gave allyltrichlorogermane as the main product upon heating above 180°. Products arising from thermolysis at reduced pressure showed that both GeCl and GeC bonds are labile as well as the remote carbon-chlorine bond.

The crystal structure of (hydrogen ethylenediaminetetraacetato)-aquoferrate(III) has been determined using three dimensional x-ray diffraction data. There are four molecules in the monoclinic unit cell, spacegroup P21/c with dimensions, a = 8.36, b = 8.94, c = 17.83 Å, β = 99.5°. In the struct...

Two dibenzoylmethane (DBM) derivatives with methyl (Me-DBM) or carbazole (CBZ-DBM) substituents at the para-position of the phenyl ring and their four novel ternary and tetrakis Eu3+ complexes with 1,10-phenanthroline (PHEN) as a secondary ligand or tetraethylamonium ion (N+(Et)4) as the counter...

In this work, one novel carbazole side chained benzodithiophene (BDT) monomer is designed and synthesized, and this new donor monomer based two D−A conjugated polymers with electron-withdrawing acceptor 4,7-di(4-(2-ethylhexyl)-2-thienyl)-5,6-difluoro-2,1,3-benzothiadiazole (DTffBT) (P5) and benz...