The protected β-nucleosides 1-(2,4,6-tri-O-acetyl-3-deoxy-3-fluoro-β-d-glucopyranosyl)-N4-benzoyl cytosine (2a) and 9-(2,4,6-tri-O-acetyl-3-deoxy-3-fluoro-β-d-glucopyranosyl)-N6-benzoyl adenine (2b), were synthesized by the coupling of peracetylated 3-deoxy-3-fluoro-d-glucopyranose (1) with s...

A series of methoxy- and fluoro-pyridines have been deprotometalated in tetrahydrofuran at room temperature by using a mixed lithium–zinc combination obtained from ZnCl2·TMEDA (TMEDA=N,N,N′,N′-tetramethylethylenediamine) and LiTMP (TMP=2,2,6,6-tetramethylpiperidino) in a 1:3 ratio, and the m...

In this work libraries of morpholines and oxazepanes have been prepared via the reductive amination reaction between dialdehydes, derived from carbohydrates, and a range of amines. In this way, functionalised morpholines and oxazepanes have been prepared that include N-alkylated derivatives, dis...

A one-pot, four-component reaction of ethyl acetoacetate, hydrazine hydrate, aldehydes, and malononitrile was discussed using Lewis acid catalyst morpholine triflate (MorT) to afford a series of dihydropyrano[2,3-c]pyrazoles, which were generally catalyzed by organic alkalis. Moderate to excelle...

Drugs affecting more than one target could result in a more efficient treatment of multifactorial diseases as well as fewer safety concerns, compared to a one-drug one-target approach. Within our continued efforts towards the design of multifunctional molecules against atherosclerosis, we hereby...

Substituted morpholines have been efficiently synthesised in good yields from nitrogen tethered alkanol-epoxide mediated by boron trifluoride etherate. The methodology has been used for the total synthesis of (±)-viloxazine.

The synthesis of methyl N-(4-nitrophenyl)-3-oxomorpholine-2-carboxylate and ethyl N-(4-nitrophenyl)-2-oxomorpholine-3-carboxylate, via rhodium(II) acetate catalyzed intermolecular O–H and intramolecular N–H carbene insertion, is described. The products represent new and versatile building bloc...

In the present study, a novel series of Schiff bases of 4-(4-aminophenyl)-morpholine were synthesised and characterised by IR, 1H-NMR, 13C-NMR, Mass spectral and elemental analysis. The compounds were screened for antibacterial (Staphylococcus aureus (ATCC 9144), Staphylococcus epidermidis (ATCC...

Development of novel anticancer drugs is inevitable to improve treatment of cancers. In this study, novel derivatives of indoline and morpholine were synthesized and tested for their cytotoxic effects on osteosarcoma and Human Embryonic Kidney cells. To characterize cytotoxicity and the mechanis...

The discovery and SAR of potent, selective dioxane-fused tricyclic benz[d]imidazole derivatives as mPGES-1 inhibitor are herein described. Various amide modifications in this series afforded many potent mPGES-1 inhibitors, of which 17d proved to be suitable for further profiling in vivo. Compoun...

A series of novel fused heterocycle methyl esters were designed and synthesized as human nonpancreatic secretory phospholipase A2 (hnps-PLA2) competitive inhibitors. Among the 22 synthesized compounds, 17 quinoline-4-methyl esters displayed hnps-PLA2 inhibition activity in the in vitro bioassay....

A series of photosynthetic electron transport (PET) inhibitors from the group of salicylanilide alkylcarbamates was investigated. The compounds were analyzed using RP-HPLC to determine lipophilicity, and their PET inhibition was determined in spinach (Spinacia oleracea L.) chloroplasts. The site...

A novel series of sulfonamide derivatives 4–21 have been synthesized starting from the strategic starting material (E)-4-Chloro-N-(4-(1-(2-(2-cyanoacetyl)hydrazono)ethyl)phenyl) benzenesulfonamide 4. Two series of hydrazone 5–9, and pyridone 10–21 derivatives bearing a sulfonamide moiety were...

IntroductionGrade IV vestibular schwannoma (Koos classification) is generally considered to be an indication for microsurgical resection or combined radiosurgery-microsurgery. However, the place of Gamma Knife stereotactic surgery (GK-SRS), either as first-line treatment or when progression of r...

The delayed protective effect of GK-2, a dipeptide mimetic of Nerve Growth Factor, was investigated on the model of focal one-sided traumatic brain injury (TBI) of the sensorimotor cortex region on the 180th day after the injury. TBI caused a reliably disruption of the functions of the limbs con...

GK-1 is a parasite-derived peptide adjuvant of 18 amino acid-length that enhances T-cell function and increases survival in B16-F10 melanoma tumor-bearing mice. This study was designed to evaluate in vivo the antitumor efficacy of GK-1 on 4T1 mouse mammary carcinoma.BALB/c mice with palpable pri...

PurposeThe synthetic peptide GK-1 potentiates protective immunity elicited by the influenza vaccine in mice. In order to understand its adjuvant properties, this study was designed to determine the impact of GK-1 on gene expression and phagocytosis of peritoneal macrophages (PMa).

Until recently, deprotonative metalation reactions have been performed using organometallic compounds that contain only a single metal (eg, organolithium reagents). Since the turn of the millennium, bimetallic compounds such as alkali metal magnesiates have begun to emerge as a new class of comp...

The anionic polymerization of d,l-lactide initiated by lithium diisopropylamide.monoTHF complex was performed in different solvents and at various temperatures. No polymerization took place in THF solution. In dioxane at 25°C the polymerization is fast and goes up to completion in few minutes. ...

Diversity oriented concise asymmetric syntheses of l-2,3-trans-3,4-cis-dihydroxyproline and (3S,5S)-3,4,5-trihydroxypiperidine have been developed from (R)-glycidol. The key step of the synthesis is Sharpless asymmetric dihydroxylation on enantiomerically pure TBDMS protected allylic alcohol 14 ...