A series of new 3- and 4-ring bis(2-aminophenoxy) aromatic diamines were prepared. These, and corresponding, conventional bis(4-aminophenoxy) diamines were reacted with several aromatic bis(ether anhydride)s to form poly(ether imide)s. The diamines with 4-aminophenoxy groups gave high-molecular-...

The novel regiospecific and general reduction of 5-benzylidene-2,4-thiazolidinediones and 5-benzylidene-4-oxo-2-thiazolidinethiones to the corresponding 5-benzyl derivatives has been accomplished using lithium borohydride in pyridine and tetrahydrofuran. Sodium borohydride and lithium chloride c...

A series of thiazolidinedione based amide derivatives were designed, synthesized and docked against the PPARγ receptor target. 11 compounds from the series with good glide scores were selected for in vivo antidiabetic study based on streptozotocin induced diabetic rat model. It was observed tha...

Allosamidin is a family 18 chitinase inhibitor produced by Streptomyces. In its producing strain, Streptomyces sp. AJ9463, allosamidin promotes production of the family 18 chitinase originated from chi65 in a chitin medium through the two-component regulatory system encoded by chi65R and chi65S,...

Allosamidins, metabolites of Streptomyces with strong inhibitory activities toward family 18 chitinases, show a variety of biological activities in various organisms. We prepared photoaffinity and biotinylated probes of allosamidin and demethylallosamidin, the N-demethyl derivative that shows mu...

In the research presented we report the development of a simple and robust liquid chromatographic method for the quantification of two genotoxic alkyl sulphonate impurities (namely methyl p-toluenesulfonate and isopropyl p-toluenesulfonate) in Aprepitant API substances using the Analytical Quali...

Water/ethanol complexation inducing solubility variation of transition-metal p-toluenesulfonates (tosylates) was investigated. The solubilities of hexaquocobalt(II) bis (p-toluenesulfonate) [Co(OTs)2·6H2O] and hexaquonickel(II) bis (p-toluenesulfonate) [Ni(OTs)2·6H2O] in water/ethanol mixtures...

Two guanine nucleotide analogs, 8-(6-aminohexyl)-amino-guanosine-5′-triphosphate and 8-(6-aminohexyl)-amino-guanosine-5′-diphosphate, were synthesized from the monophosphate by phosphorylation with pyrophosphate or orthophosphate. Structural assignments were made according to nuclear magnetic ...

The nucleotide 8-(6-aminohexyl)-amino adenosine 5′-monophosphate (8-AHA-AMP) has been investigated by 220-MHz proton magnetic resonance spectroscopy. The conformation and ionization state of the nucleotide have been determined. The anti-conformation about the glycosyl bond is the preferred form...

8-(6-Aminohexyl)-amino-AMP and 8-(6-aminohexyl)-amino-NAD(H) are synthesized from AMP and NAD+, respectively, in a two-step procedure via the 8-Br-adenine nucleotides. The AMP derivatives and the NAD+ derivatives possess some biological activity as substrates in the adenylate kinase and as coenz...

8-(6-Aminohexyl) amino-cyclic ATPR, a new affinity probe for the study of cADPR-binding proteins, was prepared in four steps with an overall yield of 21%.

A series of bifunctional molecules have been synthesized which result from the combination of a DNA sequence-specific ligand (netropsin) coupled to an intercalator moiety (OPC). The binding constants to double-stranded polynucleotides as well as the cytostatic activity against both murine and hu...

The simple reversible intercalating agent isopropyl-OPC (iPr-OPC) induces frameshift-1 mutations in Salmonella typhimurium and Escherichia coli. The mutagenic responses of S. typhimurium and E. coli wild-type strains are not proportional to the amount of drug intercalated into double-stranded nu...

In a search for new antiretroviral agents acting at the nucleic acid level, two hybrid molecules composed of a bispyrrolecarboxamide chain related to netropsin, linked to the intercalating chromophore oxazolopyridocarbazole, were tested on the cycle of a defective Moloney murine leukemia virus (...

In this communication we report on our studies into the previously undetected dimerization chemistry of thiazolium salts. Thiazolium salts with electron-withdrawing substituents, such as 3,4-dimethyl-5-ethoxycarbonylthiazolium iodide, yield acid- and oxygen-sensitive ethylenic dimers under condi...

The behavior of non-metallic inclusions in LCAK (low carbon aluminum killed) steel produced by BOF (basic oxygen furnace)-LF (ladle furnace) refining-FTSC (flexible thin slab continuous caster) production route was investigated. The results showed that, LF refining for LCAK steel could decrease ...

The BOF (basic oxygen furnace) process is very complex, and the endpoint temperature and composition are influenced by many factors, therefore it is difficult to control. To accurately predict the endpoint temperature and carbon content has very important meaning for raising the endpoint hitting...

Oxygen volume control is very important in BOF (Basic Oxygen Furnace) steelmaking production. In this study, a case-based reasoning (CBR) model with mixed case retrieve and case reuse steps is adopted to calculate the oxygen volume. Two case retrieve methods are used here: KNN (k nearest neighbo...

Background and purpose5-Chloro-2,4-dihydroxypyridine (Gimeracil) is a component of an oral fluoropyrimidine derivative S-1. Gimeracil is originally added to S-1 to yield prolonged 5-FU concentrations in tumor tissues by inhibiting dihydropyrimidine dehydrogenase, which degrades 5-FU. We found th...

Solubilities of gimeracil (form P) in aqueous co-solvent mixtures of isopropanol, N,N-dimethylformamide (DMF), ethylene glycol (EG) and dimethylsulfoxide (DMSO) were investigated via the isothermal dissolution equilibrium method at (283.15–328.15) K under ambient pressure p = 101.2 kPa. Experim...