The mixed anhydride of oxalic and phosphoric acids, oxalyl phosphate, has been prepared by reaction of oxalyl chloride and inorganic phosphate in aqueous solution. The product was purified by anion exchange chromatography and characterized by 31P and 13C NMR. This acyl phosphate has a half-life ...
A glycosyltransferase gene, rhoG, involved in the biosynthesis of the anthracycline antibiotic β-rhodomycin was isolated as a 4.1-kb DNA fragment containing rhoG and its flanking region from Streptomyces violaceus by degenerate and inverse PCR. Sequencing analysis showed that rhoG was located i...
(±)-2-Acetoxy-4,11-dideoxy-10-oxo-β-rhodomycinone [(±)-6a] was synthesized from the tricyclic quinone (1) by a short efficient route in an overall yield of about 54%. Reaction of (±)-6a with protected daunosamine followed by reduction and deprotection provided the optically active α-glycosi...
The study on the photocatalytic activity of organic aerogels produced from Estonian oil shale processing by-products and doped with Fe, Ni, Cu, Zn and Co was performed for the first time in water treatment processes. The synthesis of aerogels from oil shale phenolic compounds is unique and promi...
Incorporation of halogen atoms to drug molecule has been shown to improve its properties such as enhanced in membrane permeability and increased hydrophobic interactions to its target. To investigate the effect of halogen substitutions on the antibacterial activity of trimethoprim (TMP), we synt...
The title compound 2-(6-hydroxy-1-benzofuran-3-yl) acetic acid (abbreviated as HBFAA) has been synthetized and characterized by FT-IR, FT-Raman and NMR spectroscopic techniques. Solid state crystal structure of HBFAA has been determined by single crystal X-ray diffraction technique. The crystal ...
A series of novel VEGFR-2 inhibitors containing oxime as hinge binding fragment were described. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bond was employed to mimic the planar quinazoline. The oxime group was firstly introduced to interact with hinge region of...
VEGFR-2 plays an essential role in angiogenesis and is a central target for anticancer drug discovery. In order to develop novel VEGFR-2 inhibitors, we designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results indicated that four compounds...
A remarkable attention have been devoted to fabricate blue OLEDs, since it plays a vital role in the field of organic electronics particularly in full colour flat panel displays. Though, notable research outputs were emerged, it is still being a challenging task by the researchers to fulfil its ...
Substantial effort has been devoted toward understanding the psychopharmacological effects of tryptamine hallucinogens, which are thought to be mediated by activation of 5-HT2A and 5-HT1A receptors. Recently, several psychoactive tryptamines based on the N,N-diallyltryptamine (DALT) scaffold hav...
Gram-negative bacteria are implicated in the causation of life-threatening hospital-acquired infections. They acquire rapid resistance to multiple drugs and available antibiotics. Hence, there is the need to discover new antibacterial agents with novel scaffolds. For the first time, this study e...
Direct cycloauration of 2-phenoxypyridines with different substituents at the 5-position of the pyridine ring was carried out in an CH3CN/H2O medium, leading to isolation of cycloaurated compounds AuCl2(L) (HL=substituted 2-phenoxypyridine ligand) with alkyl, substituted alkyl, phenyl, halo, est...
The photophysical properties such as singlet absorption, molar absorptivity, fluorescence spectra, fluorescence quantum yield (ϕf) and transition dipole moment (μ12) of 3-(4′-dimethylaminophenyl)-1-(2-pyridinyl) prop-2-en-1-one (DMAPP) were measured in different media. DMAPP dye exhibits a lar...
The photophysical properties of DMAPrP have been investigated in different solvents. DMAPrP dye exhibits a large change in dipole-moment upon excitation due to an intramolecular charge transfer interaction. A crystalline solid of DMAPrP give an excimer like emission at 546 nm. The ground and exc...
The role of all-trans-retinoic acid (ATRA) in the development and maintenance of many epithelial and neural tissues has raised great interest in the potential of ATRA and related compounds (retinoids) as pharmacological agents, particularly for the treatment of cancer, skin, neurodegenerative an...
Publisher SummaryThe diazines pyridazine, pyrimidine, pyrazine, and their benzo derivatives cinnoline, phthalazine, quinazoline, quinoxaline, and phenazine have played a central role in many investigations. Progress has been made on the syntheses and reactions of these heterocycles and their use...
An improved and efficient entry to highly functionalized β-(2-pyridyl)- and β-(4-pyridyl)alanines and the corresponding 1,4-dihydro and N-oxide derivatives has been developed by one-pot thermal Hantzsch-type cyclocondensation of aldehyde–ketoester–enamine systems in which one of the reagents...
Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an α-amino oxadiazolone into a representative d...
We describe the synthesis of a library of new pseudopeptides and their inhibitory activity of the rabbit 20S proteasome chymotrypsin-like (ChT-L) activity. We replaced a natural α-amino acid by an α- or a β-hydrazino acid and obtained inhibitors of proteasome up to a submicromolar range (0.7 ...
A new series of 3-phenyl-1-(1,1′-biphenyl-4-yl)-2-(1H-imidazol-1-yl)propane derivatives 2a–l (related to the antifungal bifonazole) was synthesized and tested for antimicrobial activity. A number of substituents on the phenyl ring were chosen to compare the relative biological properties with ...
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