Fifteen methyl-, nitro-, or mixed substituted N-(phenyl)-2-chloroacetamides were investigated by C1 NQR. The temperature dependence of the frequencies of the 3-methylphenyl and 2,6-dimethylphenyl derivatives were studied for the range 77 K<T<300 K. Only one co C-Cl frequency was observed for the compound with the two exceptions. For N-(2-nitro,4-chlorophenyl)-2-chloroacetamide the observed valu...

This account highlights the synthesis and applications of one of the very bulky NHC ligands, IPr* (1,3-bis(2,6-bis(diphenylmethyl)-4-methylphenyl)imidazo-2-ylidene). This ligand and some of its derivatives have been found very effective in several catalytic applications and have enabled the isolation of highly reactive organometallic complexes. More specifically, applications of this ligand in ...

The present study describes several novel 2,5-biaryl-3-hexylthiophene derivatives (3a-i) synthesized via a Pd(0)-catalyzed Suzuki cross-coupling reaction in moderate to good yields. The novel compounds were also analyzed for their anti-thrombolytic, haemolytic, and biofilm inhibition activities. In addition, the anti-tumor activity was also evaluated in vitro for newly-synthesized compounds, wh...

The analysis of [5,10-dibromo-15,20-bis(4-methylphenyl)porphyrinato]palladium(II), [Pd(C34H22Br2N4)], and [5,10-dibromo-15,20-bis(4-methylphenyl)porphyrinato](methanol)zinc(II), [Zn(C34H22Br2N4)(CH4O)], reveals a small but localized influence of the bromine residues on the conformation of the macrocycle. A comparison of the 5,10-dibromo substituent pattern with literature data for 5,15-dibromop...

Iloperidone, [1-[4-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]eth anone, 1, is currently undergoing clinical trials as a potential antipsychotic agent. The metabolism of iloperidone was studied in human liver microsomes to define the metabolic pathways and to identify the cytochrome P450 (CYP) isoforms responsible for the formation of major iloperidone metabo...

Enantiomerically pure (S,S)-1,2-bis[(o-alkylphenyl)phenylphosphino]ethanes (o-alkylphenyl = o-methylphenyl, o-ethylphenyl, o-isopropylphenyl, 5',6',7',8'-tetrahydronaphthyl), (S,S)-1,2-bis(alkyl-methylphosphino)ethanes (alkyl = t-butyl, 1-adamantyl, 1-methylcyclo-hexyl, 1,1-diethylpropyl, cyclopentyl, cyclohexyl) (abbreviated as BisP*), and (R,R)-1,1-bis(alkylmethylphosphino)methanes (alkyl = i...

Novel N-3-alkylated 6-anilinouracils have been identified as potent and selective inhibitors of bacterial DNA polymerase IIIC, the enzyme essential for the replication of chromosomal DNA in gram-positive bacteria. A nonradioactive assay measuring the enzymatic activity of the DNA polymerase IIIC in gram-positive bacteria has been assembled. The 6-anilinouracils described inhibited the polymeras...

The condensation of chlorides of substituted pyrazinecarboxylic acids with ringsubstituted anilines yielded twelve substituted pyrazinecarboxylic acid amides. The synthetic approach, analytical, and lipophilicity data of the newly synthesized compounds are presented. Two antituberculosis assays were used. Firstly, the antimycobacterial activity against four different Mycobacterium strains in a ...