An approach to the synthesis (4-di- and -trifluoroalkyl-1-alkyl-1H-pyrazol-3-yl)methylamines – promising building blocks for drug discovery and medicinal chemistry is described. The key step of the reaction sequence is fluorination of the corresponding non-symmetric trisubstituted pyrazole deri...

Amongst different amine-borane derivatives, methylamine-borane (CH3NH2BH3) seems to be one of the capable aspirants in the storing of hydrogen attributable to its high hydrogen capacity, stability and aptitude to generate hydrogen through its catalytic hydrolysis reaction under ambient condition...

The Cu(II) complexes [Cu(bpdmpz)Cl]ClO4 (1), [Cu(bdmpzp)Cl]ClO4 (2-ClO4), [Cu(bdmpzp)Cl]PF6 (2-PF6) and [Cu(tdmpza)Cl]ClO4 (3), bpdmpzp = [bis[((2-pyridylmethyl)-di(3,5-dimethyl-1H-pyrazolyl)methyl)]amine, bdmpzp = [bis((di(3,5-dimethyl-1H-pyrazolyl)methyl)-(2-pyridylmethyl)]amine and tdmpza = t...

The theoretical molecular geometry and the IR, UV, 1H and 13C NMR spectroscopic properties of 2-[2-(dimethylamino)ethyl]-6-methoxy-4-(pyridin-2-yl)-1(2H)-phthalazinone with the previously demonstrated in vivo analgesic activity were characterized. The conformational analysis, performed using the...

A novel conjugated polymer (P1) containing fluorene and ethyl 2-(2-(pyridin-2-yl)-1H-benzo[d]imidazol-1-yl)acetate (PBMA) was designed and successfully synthesized through the Sonogashira coupling reaction. P1 shows high sensitivity and selectivity for Ag+ detection in comparison to other metal ...

Herein, we report a new series of aliphatic substituted pyridyl-urea small molecules synthesized as potential modulators for amyloid beta (Aβ) induced mitochondrial dysfunction. Their blocking activities against Aβ-induced mitochondrial permeability transition pore (mPTP) opening were evaluate...

We developed a sensitive, selective and accurate method based on liquid chromatography with tandem mass spectrometry (LC–MS/MS) to determine N-terminal thymosin-β peptides of Ac-SDKP and Ac-ADKP in human plasma samples. Quantification of Ac-SDKP and Ac-ADKP was performed using solid phase extr...

A wide variety of different sialic acids have been reported in nature. Following their release and purification, detection and quantitation of these molecules is now possible by a number of techniques. We and others have previously reported high-pressure liquid chromatography separation of siali...

Chiral 3-methoxy-2,5-morpholinediones which are cyclic N,O-acetals have proved to be excellent chiral cationic amino acid equivalents, especially if larger nucleophiles are employed. They are easily obtained from dipeptolides formed between chiral α-hydroxy acids and dimethyl amino malonate via...

Cyclodepsipeptides are known to exhibit a broad spectrum of biological activities and present a great potential for pharmacological application. A novel didepsipeptide member of the family, 6-(propan-2-yl)-3-methyl-morpholine-2,5-dione, was synthesized and its structure was confirmed by IR, 1H a...

Compound 1 exhibits potent binding inhibition activity against a corticotropin-releasing factor 1 (CRF1) receptor (IC50 = 9.5 nM) and in vitro antagonistic activity (IC50 = 88 nM) but is rapidly metabolized by human hepatic microsomes (182 μL/min/mg). Here we identified metabolically stable com...

Mass transport accompanying the redox process of ferrocenyle-undecanethiol monolayers has been examined by an electrochemical quartz crystal microbalance (EQCM) for both compact and loosely packed layers with different surface coverages prepared by self-assembly method. Ferricinium cations forme...

[3+2] Cycloadditions of (1Z,4R∗,5R∗)-1-arylmethylidene-4-benzoylamino-3-oxo-5-phenylpyrazolidin-1-ium-2-ides 1a–e to methyl methacrylate gave the 1-CO2Me regioisomers 3/3′, exclusively, in 1–67% yields. Stereocontrol was dependent on the ortho-substituents at the 1′-aryl group in dipole 1: o...

New, highly functionalised (1E,3E)-1-(benzoylamino)-4-(dimethylamino)buta-1,3-diene-1,2,3-tricarboxylates proved to be useful and versatile reagents in the formation of highly substituted pyridine, N-aminopyridine, pyrrole and pyrido[3,4-c]pyridazine derivatives. The formation of the particular ...

MicroRNA-21, as an oncogenic miRNA, has caught great attention for medicinal chemists to develop its novel inhibitors for cancer therapy. In the present study, we designed 4-benzoylamino-N-(prop-2-yn-1-yl)benzamides as miR-21 inhibitor candidates on the basis of scaffold hopping. Eighteen compou...

Crystal and molecular structure of 1-phenyl-3-benzoylamino-4-benzoylpyrazol-2-in-5-one as a product of the benzoylation of 1-phenyl-3-benzoylaminopyrazol-2-in-5-one was characterised by X-ray single crystal diffraction. It is shown that 1-phenyl-3-benzoylamino-4-benzoylpyrazol-2-in-5-one exists ...

A new series of 3-benzoylamino-5-imidazol-5-yl-benzo[b]thiophenes and the parent amino derivatives were synthesized and screened as antitumor agents. All tested compounds showed concentration-dependent antiproliferative activity profile against HeLa cell line, exhibiting GI50 values in the low m...

The long-term objective is to understand the role of the adrenal ina altering systemic arterial blood pressure. This paper summarizes research on genetic hypertension in the rat and bears a relationship to several forms of human hypertension in which defects of steroid hydroxylases lead to incre...

19-Acetylenic-deoxycorticosterone (19-A-DOC) is believed to be a competitive irreversible inhibitor of the synthesis of 19-nor-deoxycorticosterone (19-nor-DOC), a potent mineralocorticoid implicated in some forms of human and animal hypertension. It has been shown to inactivate 11β/19-hydroxyla...

Highly conjugated azo-aromatic systems have been prepared in high to moderate yields by linking mono- and bis-azo aromatic fragments to 4-(Rn-azulen-1-yl)-2,6-dimethyl-pyridine. The synthesized π-extended systems have been studied by NMR spectroscopy, UV–Vis and electrochemistry. Systematic in...