2-amino-(N-d-ribosyl)acetamide 5′-phosphate (GAR, 10) has been prepared in a readily scaled-up synthesis from 2,3-O-isopropylidene-d-ribofuranosylamine p-toluenesulfonate (3) by condensation with the mixed anhydride of N-(benzyloxy-carbonyl)glycine, followed by phosphorylation with 2-cyanoethyl...

Investigations of methodologies aimed on improving the stereoselective synthesis of sialosides and the efficient assembly of sialic acid glycoconjugates has been the mission of dedicated research groups from the late 1960s. This review presents major accomplishments in the field, with the emphas...

A pyridine side-chain terminus has been incorporated into the indole-5-carboxamide and indole-5-acetamide series of GnRH antagonists. Potent activity was observed in binding and functional assays. Certain branched or cyclic tertiary amides were identified as preferred in each series. Alkylation ...

The isothiourea-catalysed chemo- and enantioselective [2,3]-sigmatropic rearrangement of N,N-diallyl allylic ammonium ylides is explored as a key part of a route to free functionalised α-amino esters and piperidines. The [2,3]-sigmatropic rearrangement proceeds with excellent diastereo- and ena...

A series of novel alkyl amide functionalized 2,3-pyrazole fused quinoline derivatives 5, 6 and 7 have been prepared starting from quinoline-2(1H)one 1 in a series of steps. All the final products were screened for antibacterial activity, the promising lead compound 5r was identified with MIC val...

A total of thirty five new N-[4-(1,3-benzothiazol-2-yl)phenyl]acetamide derivatives were synthesized and structures of all the compounds were confirmed on the basis of elemental analysis and collective use of IR, 1H NMR, 13C NMR and mass spectral data. Compounds were tested for their ability to ...

Mast cells, constituents of virtually all organs and tissues, are critical cells in IgE-mediated allergic responses. The aim of this study was to investigate the effect and mechanism of an indoxyl chromogenic compound, 5-bromo-4-chloro-3-indolyl 1,3-diacetate, CAC-0982, on IgE-mediated mast cell...

A convenient single-step synthesis of several 2,7-dimethyl-9-phenylxanthen-9-ol (DMPx-OH) analogs has been accomplished using a Friedel–Crafts reaction. Treatment of various DMPx-OH with unprotected 2′-O-methoxyethyl-ribonucleosides (MOE) in the presence of B(C6F5)3, as a Lewis Acid catalyst, ...

Two new natural compounds, astolides A,B, were isolated from Streptomyces hygroscopicus collected from the alkaline soil obtained from Saratov region, Russia. The structures were elucidated by interpretation of UV spectroscopic, MS, 1D and 2D NMR data. The relative configurations were determined...

SummaryAntibiotic-resistant bacterial pathogens pose an urgent healthcare threat, prompting a demand for new medicines. We report the mode of action of the natural ansamycin antibiotic kanglemycin A (KglA). KglA binds bacterial RNA polymerase at the rifampicin-binding pocket but maintains potenc...

Schiff base 3-((5-chloro-2-phenyl-1H-indol-3-ylimino)methyl)quinoline-2(1H)-thione and its Cu(II), Co(II), Ni(II), Zn(II) and Fe(III), complexes have been synthesized and characterized by elemental analysis, UV–Visible, IR, 1H NMR, 13C NMR and mass spectra, molar conductance, magnetic susceptib...

The effect of the pentapeptide H-Cys-Tyr-Ile-Gln-Asn-OH to act like melanocyte-stimulating hormone-releasing factor (MSH-RF) was studied. This peptide decreases at ng amounts the MSH content of the rat pituitary and increases plasma MSH concentration. This agent also stimulates the release of MS...

β-(Tyr9)melanotropin-(9–18), which itself has no analgesic action, as measured by the tail-flick and hot-plate methods, decreased morphine-induced analgesia following intracerebroventricular injection. H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH heptapeptide, which has weak CRF-like activity, had no acti...

The effects of H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH, a hypothalamic heptapeptide with weak CRF activity were investigated on the in vitro uptake and release of radiolabelled dopamine (DA), noradrenaline (NA) and serotonin (5-HT) in rat brain hypothalamic slices. In a doses of 5×10−6 M and 10−5 M th...

In the present study the role of the central dopaminergic systems in the behavioral action of H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH was investigated. The heptapeptide inhibited the extinction of active avoidance behavior if the treatment was performed intracerebroventricularly (icv) in a dose of 1 μ...

Ajuga bracteosa Wall ex. Benth. (Lamiaceae) commonly known as Bungle Weed has been in use since ancient times and is mentioned Ayurvedic literature. The upper ground parts of the plant are used for treatment of various diseases. The weed is credited with astringent, febrifugal, stimulant, aperie...

The comparative study of different hydrothermal treatment techniques (Reflux (R) and Teflon (T)) and without hydrothermal technique (W) towards efficient CO2 methanation over Ni/SBA-15 was discussed. X-ray diffraction (XRD), inductive coupling plasma-atomic emission spectroscopy (ICP-AES), N2 ad...

BackgroundMultidrug-resistant Shigella isolates have recently emerged as a serious public health threat worldwide. In particular, overseas travel is a risk factor for acquisition of antimicrobial-resistant Shigella strains. To explore the role of travel in the spread of cefotaxime-resistant Shig...

A series of spherical mesoporous Ni/Dendritic Fibrous SBA-15 (Ni/DFSBA-15) catalysts with different Ni loadings (3–15 wt.%) were successfully synthesized and catalytically investigated by methane dry reforming. The XRD and Raman analyses indicated the structural stability of DFSBA-15 regardless...

BackgroundEarly prognostication in post-cardiac arrest (CA) patients remains challenging and biomarkers have evolved as helpful tools in risk assessment. The stress-response cytokine growth differentiation factor-15 (GDF-15) is dramatically up-regulated during various kinds of tissue injury and ...