Ruthenium(II)-2, 2′-bipyridine/1, 10-phenanthroline complexes incorporating (E)-2-(((5-((4-methoxyphenyl)ethynyl)pyridin-2-yl)imino)methyl)-4-((4-nitro phenyl)ethynyl)phenol as a ligand

Transition Metal Chemistry - A new series of hexa-coordinated Ru(II) complexes of the type [Ru(L)(phen)2]X (1a–d) and [Ru(L)(bipy)2]X (2a–d) (where...     

Furan‐Derived Chiral Bicycloaziridino Lactone Synthon: Collective Syntheses of Oseltamivir Phosphate (Tamiflu), (S)‐Pipecolic acid and its 3‐Hydroxy Derivatives

A unified synthetic strategy for oseltamivir phosphate (tamiflu), (S)‐pipecolic acid, and its 3‐hydroxy derivatives from furan derived common chiral bicycloaziridino lactone synthon is described here. Key features are the short (4‐steps), enantiopure, and decagram‐scale synthesis of common chiral synthon from furan and its first‐ever application in the total synthesis of biologically active compounds by taking the advantages of high functionalization ability of chiral synthon.     

Identification of metabolites of novel Anti‐MRSA fluoroquinolone WCK 771 in mouse,rat, rabbit,dog, monkey and human urine using liquid chromatography tandem mass spectrometry

WCK 771 is an l ‐arginine salt of levonadifloxacin (LND) being developed in intravenous dosage form and has recently completed a phase III trial in India. The pharmacokinetics of WCK 771, a novel anti‐MRSA fluoroquinolone, were examined in mice, rats, rabbits, dogs, monkeys and humans after systemic administration during pre‐clinical and clinical investigations. Urine and serum were evaluated for identification of metabolites. It was observed that LND mainly follows phase II biotransformation pathways. All of the species showed a different array of metabolites. In mice, rabbit and dog, the drug was mainly excreted in the form of O‐glucuronide (M7) and acyl glucuronide (M8) conjugates, whereas in rat and human major metabolite was sulfate conjugate (M6). Monkeys exhibited equal distribution of sulfate (M6) and glucuronide conjugates (M7, M8). In addition to these three major phase II metabolites; five phase I oxidative metabolites (M1, M2, M3, M4 and M5) were identified using liquid chromatography tandem mass spectrometry. Out of these eight metabolites M2, M3, M5, M7 and M8 are reported for the first time.     

Design and Development of Axially Chiral Bis(naphthofuran) Luminogens as Fluorescent Probes for Cell Imaging

Designing chiral AIEgens without aggregation-induced emission (AIE)-active molecules externally tagged to the chiral scaffold remains a long-standing challenge for the scientific community. The inherent aggregation-caused quenching phenomenon associated with the axially chiral (R)-[1,1′-binaphthalene]-2,2′-diol ((R)-BINOL) scaffold, together with its marginal Stokes shift, limits its application as a chiral AIE-active material. Here, in our effort to design chiral luminogens, we have developed a design strategy in which 2-substituted furans, when appropriately fused with the BINOL scaffold, will generate solid-state emissive materials with high thermal and photostability as well as colour-tunable properties. The excellent biocompatibility, together with the high fluorescence quantum yield and large Stokes shift, of one of the luminogens stimulated us to investigate its cell-imaging potential. The luminogen was observed to be well internalised and uniformly dispersed within the cytoplasm of MDA-MB-231 cancer cells, showing high fluorescence intensity.     

Transport and mechanical behavior in PEO-LLZO composite electrolytes

Journal of Solid State Electrochemistry - Composite solid electrolytes (CEs), wherein ion-conducting polymer and ceramic/glass is mixed, are promising candidates for all-solid-state batteries due...     

General Functionalization Method for Synthesis of α-Functionalized Polymers by Combination of Anionic Polymerization and Hydrosilation Chemistry

A new general functionalization method (GFM) of synthesizing α-functionalized polymers has been developed. α-Vinyl-functionalized polystyrene was obtained by anionic polymerization of styrene using 4-pentenyllithium as an initiator. Chloromethyldimethylsilane-functionalized polystyrene was successfully synthesized from vinyl-functionalized polystyrene by hydrosilation using Karstedt's catalyst. Nucleophilic substitution of this polymer was carried out in presence of pyrrolidine to obtain α-pyrrolidine-functionalized polystyrene. α-Triethoxysilylpolystyrene was obtained by hydrosilation of a-4-pentenylpolystyrene with triethoxysilane using Karstedt's catalyst.     

Stereoselective synthesis of (-)-1-epi-ventiloquinone L and (+)-ventiloquinone L, the monomeric unit of cardinalin 3

A stereoselective synthesis of (-)-1-epi-ventiloquinone L and (+)-ventiloquinone L, the monomeric unit of cardinalin 3 has been described. The synthesis is completed in 7 steps with 10.5% and 13% overall yields for (-)-1-epi-ventiloquinone L and (+)-ventiloquinone L respectively. The key steps involve D?tz benzannulation of carbene 5 with alkyne 6 to give a substituted naphthalene moiety and oxa-Pictet-Spengler reaction to install the 1,3-dimethylpyran moiety.     

Concise and practical route to tri- and tetra-hydroxy seven-membered iminocyclitols as glycosidase inhibitors from d-(+)-glucurono-γ-lactone

An efficient and short total synthesis of tetrahydroxy-1c and trihydroxy-azepane 1d is reported in 72% and 57% overall yields, respectively, from d-(+)-glucurono-γ-lactone. Thus, d-glucuronolactone 2 on acetonide protection, DIBAL-H reduction and one-pot intermolecular reductive amination followed by -NCbz protection afforded 6-(N-benzyl-N-benzyloxycarbonyl) amino-6-deoxy-1,2-O-isopropylidene-α-d-gluco-1,4-furanose 5a. 1,2-Acetonide hydrolysis in 5a and Pd-mediated intramolecular reductive aminocyclization afforded tetrahydroxyazepane 1c. An analogous pathway with 5-deoxy-1,2-O-isopropylidene-α-d-glucurono-6,3-lactone 3b gave trihydroxy-azepane 1d. Glycosidase inhibitory activity of 1c/1d was studied and 1d was found to be potent inhibitor of α-mannosidase and β-galactosidase.     

Determination of track registration efficiency and radiation chemical yield for loss of ester bonds due to gamma rays in Cellulose Acetate Butyrate (CAB) nuclear track detector

The fission track registration efficiency of an indigenously prepared Cellulose Acetate Butyrate (CAB) solid state nuclear track detector (SSNTD) has been determined and is found to be (0.89 ± 0.04). Radiation chemical yield, G-value for loss of ester bonds in this detector exposed to gamma rays from a Co-60 source has also been determined by FT-IR spectrometry. The amount of ester bonds lost due to the exposure was estimated from the change in absorbance of C=O and C–O–C bonds with the gamma dose. The G-value for breaking of ester bonds in CAB detector is found to be about 37/100 eV.