Synthesis of various fused heterocyclic rings from thiazolopyridine and their pharmacological and antimicrobial evaluations

Various fused-heterocyclic-derivatives containing thiazolopyridine moieties has been synthesized by allowing 5-aminothiazolo[3,2-a]pyridine derivative 1 to undergo annulations reactions with different reagents under different-reaction conditions. The biological assessment of compounds 2 , 11 , 14 , 15 , and 19 showed remarkable antimicrobial activities. In addition, selected derivatives of the products were screened for their anticancer activities against two tumor cell lines using MTT assay and the results showed that some of these compounds have potent cytotoxic effect, as concluded from their IC₅₀ values. Meanwhile, compounds 3a , 7 have exhibited very strong potency as anticancer candidates. Thiazolopyridine structures have been confirmed as a useful lead compounds for the development of new anticancer agents. Molecular docking showed that,-some of the synthesized compounds more suitable inhibitor against-ALR2 with farther alteration in future.     

Local Thermodynamic Description of Isothermal Single-Phase Flow in Simple Porous Media

Transport in Porous Media - Darcy’s law for porous media transport is given a new local thermodynamic basis in terms of the grand potential of confined fluids. The local effective pressure...     

Supramolecular polymer gels from polystyrene bearing cyclic amidine Group and acrylic acid/n‐butyl acrylate copolymers

We have prepared supramolecular polymer gels by mixing solutions of a polystyrene bearing cyclic amidine pendant groups (Poly‐A) and copolymers of acrylic acid and n‐butyl acrylate (Poly‐C), followed by evaporation. FT‐IR analysis indicated that the gels were formed through three‐dimensional network of the amidinium‐carboxylate salt bridge. DSC study showed that the Poly‐A and the Poly‐C were miscible when the salt bridge content was high. On the other hand, the mixtures with small salt bridge content showed phase separation. Dynamic shear measurements showed that the gel prepared from Poly‐A and Poly‐C with acrylic acid unit content of 15% had G' higher than G″ over a temperature range of ?22 °C to 32 °C, in which the G' value reached almost 1 MPa. The gel had a crossover point of G' and G″ at 32 °C, very close to room temperature, which suggested facile processability. © 2015 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2016 , 54, 765–770     

Effect of three vitrification methods on development of two-cell mouse embryos

The purpose of this study was to investigate the effect of three vitrification procedures [conventional straw (CS), open pulled straw (OPS) and closed pulled straw (CPS)] on the development of two-cell mouse embryos. Two-cell mouse embryos were randomly divided into vitrified and non-vitrified control groups. Embryos in the vitrified group were cryopreserved within a combination of 5.5 M ethylene glycol and 1M sucrose as cryoprotectants, loaded within three different straws (CS, OPS and CPS) and warmed in stepwise sucrose solutions. The survived embryos from each procedure were cultured in human tubal fluid (HTF). The non-vitrified control embryos were also cultured in the same manner. The rates of the development in all the groups were daily determined and statistically compared. On day 4 of the cultivation period, several expanded blastocysts from each group were randomly selected and stained either with propidium iodide (PI) and bisbenzimide or with terminal transferase- mediate DNA end labeling (TUNEL) Technique. The mean number of the inner cell mass (ICM), trophoectoderm (TE), necrotic and apoptotic cells were counted and statistically compared. The survival rate of embryos in CPS was significantly higher than that in OPS and CS. The rate of hatched blastocysts did not differ in the three vitrification procedures, but in comparison with that of the control, CS and OPS showed a significant reduction. The mean number of ICM and TE decreased in CS and OPS, whereas in CPS it was almost identical to that of the control. The incidence of apoptosis and necrosis appeared to be almost similar in all the groups. In conclusion, CPS seems to be an effective, easy and rapid method for the cryopreservation of two-cell mouse embryos.     

In vivo mapping of functional domains and axonal connectivity in cat visual cortex using magnetic resonance imaging

Noninvasive cognitive neuroimaging studies based on functional magnetic resonance imaging (fMRI) are of ever-increasing importance for basic and clinical neurosciences. The explanatory power of fMRI could be greatly expanded, however, if the pattern of the neuronal circuitry underlying functional activation could be made visible in an equally noninvasive manner. In this study, blood oxygenation level-dependent (BOLD)-based fMRI and diffusion tensor imaging (DTI) were performed in the same cat visual cortex, and the foci of fMRI activation utilized as seeding points for 3D DTI fiber reconstruction algorithms, thus providing the map of the axonal circuitry underlying visual information processing. The methods developed in this study will lay the foundation for in vivo neuroanatomy and the ability for noninvasive longitudinal studies of brain development.     

Synthesis,characterization, and molecular structures of Ni(II) and Cd(II) complexes derived from dithiophosphonate

Two novel dithiophosphonate ligands, HS₂P(p‐C₆H₄OMe)(OCH₂CH₂CH(CH₃)₂) ( 1 ) and HS₂P(p‐C₆H₄OMe)(OCH(CH₃)₂) ( 2 ), were synthesized and characterized by multinuclear (¹H, ³¹P, and ¹³C) NMR, infrared spectroscopy as well as elemental analysis. The reactions of 1 and 2 with NiCl₂·6H₂O and Cd(NO₃)₂·4H₂O in methanol led to novel complexes 3 and 4 . The single crystal X‐ray structures of 3 and 4 showed tetracoordinated structure with square planar geometry for the nickel complex, while it showed pentacoordinated structure with distorted square‐pyramid environment for the cadmium complex.     

Keggin Heteropolyacid Catalyzed Synthesis of Isoxazolo[5,4-d]pyrimidine-4,6(5H,7H)-diones at Room Temperature

Isoxazolo[5,4‐d]pyrimidine‐4,6(5H,7H)diones 2a – 2f have been synthesized from the reaction of ethyl 5‐amino‐3‐methyl‐4‐isoxazole carboxylate ( 1 ) with aryl isocyanates in the presence of Keggin heteropolyacid H₃[PW₁₂O₄₀] as a green solid acid catalyst at room temperature in a one‐pot process in good yields.     

Efficient and solvent-free synthesis of 1-amidoalkyl-2-naphthols using <Emphasis Type="Italic">N,N,N’,N’</Emphasis>-tetrabromobenzene-1,3-disulfonamide

N,N,N,’N’-Tetrabromobenzene-1,3-disulfonamide [TBBDA] is found to be a reusable catalyst for efficient synthesis of various amidoalkyl naphthols from β-naphthol, aromatic aldehydes and urea in good to high yields under solvent-free conditions.