Conversion of (5S)-N-(tert-butoxycarbonyl)-5-(methoxycarbonyl)-2-pyrroline to its corresponding amide, an important intermediate in the synthesis of the dipeptidyl peptidase IV (DPP4) inhibitor Saxagliptin, was carried out by ammonolysis reaction catalyzed by immobilized Candida antarctica lipas...

Anti-inflammatory/analgesic 3,3′-(1,2-ethanediyl)-bis[2-(3,4-dimethoxyphenyl)-4-thiazolidinones] 1, obtained as racemic mixtures (a) and mesoforms (b), have two equivalent stereogenic centres (C-2 and C-2′) and exist as RR, SS and RS isomers. The enantioseparation of 1a provided the single ena...

In order to study dependence of enantioseparation capability on structure of chiral selectors derived from N-cycloalkylcarbonyl chitosan, nine chitosan 3,6-bis(arylcarbamate)-2-(cyclopentylformamide)s were synthesized. The corresponding chiral stationary phases (CSPs) were prepared with the chit...

The enantioselective total synthesis of the diyne containing natural products panaxytriol and (3S,10R)-panaxydiol from l-tartaric acid is reported. Key steps in the synthesis include the elaboration of a γ-hydroxy amide derived from tartaric acid to the required alkyne and the formation of the ...

Using a classical hybridization approach, a series of 1H-benzo[d]imidazoles and 3,4-dihydroquinazolin-4-ones were synthesized (39 examples) and evaluated as inhibitors of Mycobacterium tuberculosis growth. Chemical modification studies yielded potent antitubercular agents with minimum inhibitory...

In this study, catecholamides (7a–l) bearing different aromatic rings (such as pyridine-2-yl, pyridine-3-yl, phenyl, and 2-chlorophenyl groups) were synthesized as potent phosphodiesterase (PDE) 4 inhibitors. The inhibitory activities of these compounds were evaluated against the core catalytic...

A novel series of tubulin polymerization inhibitors, based on fluorinated derivatives of isocombretastatin A-4 was synthesized with the goal of evaluating the effect of these compounds on the proliferative activity. The introduction of fluorine atom was performed on the phenyl ring or at the lin...

The synthesis of multisubstituted 4-nitrobuta-1,3-dien-1-amines (nitrodienamines) from 3-aminocrotonates and nitroacetaldehyde potassium salt, has been performed in 45–89% yields. This one-step protocol works efficiently with a broad range of N-H and N-substituted 3-aminocrotonates and delivers...

An efficient chemoenzymatic synthesis of (−)-3-methyl 5-(2-propoxyethyl) (4R)-4-[2-(difluoromethoxy)phenyl]-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylate has been achieved. The key step is a highly stereoselective Candida rugosa lipase (CRL)-mediated asymmetrisation of the prochiral bis[(is...

The uniform microrods, microspikes, and monodispersed microspheres of 1,2-diphenyl-4-(4-methoxyphenyl)-1,3-cyclopentadiene (PMPCP) were prepared by a facile solvent evaporation method. The effect of reaction conditions on the morphology evolution of PMPCP aggregates was investigated. It is belie...

In the present work, complex formation equilibria between copper(II) and 1,1,1-trifluoro-4-(2-methoxyphenyl)butan-2,4-dione (1) have been investigated by UV–vis spectroscopy in ethanol/0.01 M NEt4NO3 as an ionic strength adjuster at 25 °C. The composition of the complex in solution was determi...

In this paper diethyl (hydroxy(4-methoxyphenyl) methyl) phosphonate has been synthesized and characterized by FTIR, FT-Raman UV–Vis. The structural geometrical parameters, vibrational, electronic, HOMO-LUMO, Fukui analysis, and the thermodynamic properties of the molecule were performed on the ...

A novel organic nonlinear optical material 1-(4-methylphenyl)-3-(4-methoxyphenyl)-2-propen-1-one has been synthesized by the standard method. The synthesized compound was purified by repeated re-crystallization. FT-IR spectra was recorded to identify the various functional groups present in the ...

In order to improve the modest oral activity of PGE2 as an inhibitor of gastric acid secretion, analogs were prepared and tested orally in histamine-challenged rats. Insertion of a double bond at C-4, resulting in the 4,5-allene analog of PGE1, gave a small increase in activity. Introduction of ...

SummaryPlastoquinones play important roles as electron carriers in the light-dependent reactions of photosynthesis and also as a cofactor of phytoene desaturation in the synthesis of carotenoid. A plastoquinone-9 (PQ-9) was identified in Frey-Wyssling organelles of fresh rubber latex from Hevea ...

The Bj1 gene encodes the Drosophila homolog of RCC1, the guanine-nucleotide exchange factor for RanGTPase. Here, we provide the first phenotypic characterization of a RCC1 homolog in a developmental model system. We identified Bj1 (dRCC1) in a genetic screen to identify mutations that alter cent...

To test the involvement of the telomeres in the senescent phenotype, we used telomerase-immortalized human foreskin fibroblasts (hTERT-BJ1). We exposed hTERT-BJ1 and parental BJ cells to either UVB or H2O2 subcytotoxic stress(es). Both cell lines developed biomarkers of replicative senescence: l...

A facile one-pot synthesis of 3-aminoquinolines from ortho-aminobenzaldehydes was developed. Ethyl 6,7-dimethoxy-3-aminoquinoline-2-carboxylate, a key intermediate for the preparation of a 4-anilino-benzo[b][1,5]-naphthyridine-3-carbonitrile, was efficiently prepared by this method. Synthetic ro...

N-Alkyl acryloylamides derived from o-aminobenzaldehyde derivatives react with N-alkyl glycine derivatives to provide cis-fused pyrrole[3,2-c]quinolones in moderate yield and high diastereoselectivity. These same substrates engage in a tandem Michael–Mannich pathway on treatment with a secondar...

Four different double metal cyanides (NiHCFe, CrHCFe, MnHCFe and ZnHCFe) were synthesized, followed by adsorbed on silica gel and used as Lewis acid catalyst in the isomerisation of substituted 2′-hydroxychalcones to flavanones under solvent-free (dry) condition. Optimization of the reaction co...