Via a five-step-reaction procedure for the preparation of 19 known N-[2-chloro-9-(tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters (6a–s) and successive removal of 9-(tetrahydropyran-2-yl) and benzylester groups 19 novel N-[2-chloro-9H-purin-6-yl]-N-cyclopropylgly...

A molecule 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine plays a significant role in the treatment of hypertension and acts as a potential I 1 imidazoline receptor agonist. In this present work, the molecular structure of the title compound has been investigated u...

A series of novel N′-tert-butyl- N′-substitutedbenzoyl-N-5-chloro-6-chromanecarbohydrazide derivatives were synthesized, and their larvicidal activities against Oriental armyworm were evaluated. The results of bioassays indicated that most of these title compounds exhibit higher larvicidal act...

The synthesis, the NMR characterization and the crystal structure of 6-Chloro 4,4′-dimethyl 2,2′-bipyridine and of the reaction intermediate 4,4′-Dimethyl 2,2′-bipyridine N-Oxide are here reported. The target compound crystallizes in the orthorhombic system while the intermediate is monoclin...

N‑(6‑Aminohexyl)‑5‑chloro‑1‑naphthalenesulfonamide (W-7), a kind of adjuvant chemotherapy, can bind to calmodulin and inhibit Ca2+/calmodulin-regulated enzyme activities and cell proliferation. Similar to calmodulin, euplotes octocarinatus centrin (EoCen) belongs to EF-hand superfamily of calciu...

A convenient synthesis of N,N-disubstituted 4H-3,1-benzothiazin-2-amines from aryl(2-isothiocyanatophenyl)methanones using a two-pot procedure has been developed. Thus, treatment of these isothiocyanato ketones with secondary amines gave the corresponding keto thioureas, which were allowed to re...

A series of nonplanar tetraphenylethene (TPE)–bis(indolyl)methane (BIM) conjugates were designed and prepared and characterized by standard spectroscopic techniques. The properties of TPE-BIM derivatives were investigated by UV/Vis and fluorescence spectroscopy, and DFT calculations. All of the...

BackgroundFalcipain 2 (FP-2) is the hemoglobin-degrading cysteine protease of Plasmodium falciparum most extensively targeted to develop novel antimalarials. However, no commercial antimalarial drugs based on FP-2 inhibition are available yet due to the low selectivity of most FP-2 inhibitors ag...

Three series of novel 3,5-bis(arylmethylene)-1-(N-(ortho-substituted aryl)maleamoyl)-4-piperidones, designed as simplified analogs of curcumin with maleic diamide tether, were synthesized and bioevaluated. These compounds displayed potent cytotoxicity towards human Molt 4/C8 and CEM T-lymphocyte...

Chlorinated carboxylic acids of fatty acid character have been shown to account for up to 90% of the extractable, organically bound chlorine (EOCl) in fish. To facilitate the detection of chlorinated fatty acid methyl esters (FAMEs) released from fish lipids, an enrichment was performed by remov...

The first NMR study of a 27-nor-triterpene of the β-amyrin type is described. In addition to conventional 1D NMR methods, 2D shift-correlated NMR techniques (DQF COSY, TOCSY, HMQC and HMBC) were used for the complete 1H and 13C NMR resonance assignments of 27-nor-olean-13-en-3-acetyloxy-28-oic ...

The synthesis of new N,N-dimethyl carbamoyl 5-aryloxytetrazoles have been reported. Their dynamic 1H-NMR via rotation about CN bonds in moiety of urea group [a; CO-NMe2 and b; (2-tetrazolyl)N-CO rotations] in the solvents CDCl3 (223–333 K) and DMSO (298–363 K) is studied. Accordingly, the free...

Electrochemical reductions of 2,2,2-trichloroethylideneacetophenones under constant cathodic potential in anhydrous acetonitrile–lithium perchlorate followed by addition of water led to previously unknown (2SR,3SR)-1,5-diaryl-2-(2,2-dichlorovinyl)-3-(trichloromethyl)pentane-1,5-diones in high t...

This paper reports one-pot synthesis of 2,2,2-trifluoroethyl 1H-pyrazole-5(3)-carboxylates via cyclocondensation of 1,1,1-trichloro-4-alkoxy-3-alken-2-ones [Cl3CC(O)C(R2) = C(R1)OMe, where R1 = H, CH3, n-octyl, n-nonyl, n-decyl, n-undecyl, n-tridecyl, −(CH2)2Ph, 4-ClC6H4, 4-BrC6H4 and R2 = H] an...

Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate...

A dihydropyridone-mediated approach to the morphine skeleton was investigated. The hexahydroisoquinoline 2 was synthesized in nine steps using N-acylpyridinium chemistry and dihydropyridone functionalization methods. This new approach should be useful in the design of more efficient syntheses of...

Graft copolymerization is a challenging step in preparation of starch-based adhesive due to the complexity and instantaneity. A combination of both experimental and simulation methodology has been employed to investigate the process at microscopic level. Through a series of characterizations of ...

Lack of suitable draw solutes is one of the major limiting factors hindering commercial realization of forward osmosis (FO) desalination process. This study investigates the feasibility of ferric sulfate as draw solute in FO desalination. A laboratory-scale, cross-flow FO apparatus utilizing com...

A simple, accurate, and fast flow-batch procedure employing photometric detection for the determination of sulfate in fuel ethanol was developed. After the formation of soluble barium sulfate in alcoholic medium, the remaining barium forms a product with dimethylsulfonazo III (DMS), the absorban...

Simple and efficient methods are described for the separation of biologically active ascorbigen and 1′-methylascorbigen by normal-phase TLC, conventional as well as new personal overpressured layer chromatographic (OPLC) systems using the same eluent. Results obtained with these techniques were...