The synthesis of 1-(4-substituted)butyl derivatives of amides of 7-methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid and the results of the preliminary pharmacological screening are described in this paper. Some of them showed a weak analgesic action and cause...

The synthesis of N-substituted oxaziridines bearing an α-(trifluoromethyl)benzyl substituent at C(3) was achieved by m-CPBA oxidation of the corresponding 3-imino-1,1,1-trifluoro-2-arylpropan-2-ols and their trimethylsilyl protected derivatives, respectively. In all cases, mixtures of diastereo...

α-Trifluoromethyl benzyl alcohol (F) was introduced as a “shift reagent” in the buffer gas of an electrospray ionization ion mobility spectrometer coupled to a quadrupole mass spectrometer to explain the mobility shifts of selected compounds; ion mobilities depended on ion sizes and F-ion add...

An efficient synthetic route towards the synthesis of β-keto sulfones has been developed from secondary benzyl alcohols using N-bromosuccinimide (NBS). The present protocol utilizes NBS as oxidant as well as brominating agent, readily accessible benzyl alcohols and sodium arenesulfinates as the...

Elevated serum interleukins (IL-6, IL-1β) over baseline concentration help in blastocyst adhesion to the uterine endometrium in the early phase of pregnancy. A nano PLA (Piperolactam A)-HPBCD (2-hydroxy-propyl-β-cyclodextrin) inclusion complex was developed as an interleukin down-regulator tha...

Scropolioside A, an iridoid isolated from Scrophularia auriculata ssp. pseudoauriculata, showed anti-inflammatory properties against different experimental models of delayed-type hypersensitivity. This iridoid reduced the oedema induced by oxazolone by 79% (72 h) at 0.5 mg/ear while reducing tha...

A series of novel 6-phenylaminopurines have been efficiently synthesized in 3 steps exploring different groups at positions 2, 8 and 9 of the purine ring and at the exocyclic nitrogen atom at position 6. Among the newly described purines, five compounds showed antiproliferative activity with IC5...

We describe the simple and fast preparation of a new radioiodinated probe for the detection of the estrogen receptor (ER) and its isoforms. Iodotamoxifen aziridine was labeled with iodine 125 ([125I]TAZ) in position 4 of the α aromatic ring. The yield was high (>75%), the label was stable and t...

The isolation of geranyl geranyl pyrophosphate synthetases from carrot root and pig liver and the properties of these enzymes are reported. Each of the enzymes catalyzes the formation of geranyl geranyl pyrophosphate from isopentenyl-4-C14 and farnesyl pyrophosphates. The product of the reaction...

When inhibitors of enzymes that utilize isoprenoid pyrophosphates are based on the natural substrates, a significant challenge can be to achieve selective inhibition of a specific enzyme. One element in the design process is the stereochemistry of the isoprenoid olefins. We recently reported pre...

A cell-free enzyme system, which catalyses the incorporation of radiolabel from [12-14C]isopentenyl pyrophosphate into the sesquiterpenoid phytoalexin lubimin, has been prepared from tuber tissue of Solanum tuberosum inoculated with an elicitor preparation from Phytophthora infestans. Biosynthes...

SummaryFarnesyl pyrophosphate (FPP) synthase catalyzes the biosynthesis of geranyl pyrophosphate (GPP) and FPP, which are the precursors of terpenoids such as essential oils, from isopentenyl pyrophosphate (IPP) and dimethylallyl pyrophosphate (DMAPP). gDNA and cDNA encoding hop (Humulus lupulus...

Farnesyl pyrophosphate synthase (FPPS) is the major molecular target of nitrogen-containing bisphosphonates (N-BPs), used clinically as bone resorption inhibitors. We investigated the role of threonine 201 (Thr201) and tyrosine 204 (Tyr204) residues in substrate binding, catalysis and inhibition...

A new series of 8-(p-substituted-phenyl/benzyl)xanthines has been synthesized and evaluated in vitro for adenosine receptor binding affinity and in vivo for bronchospasmolytic effects. It was observed that the nature of substituent at para-position of 8-phenyl/benzyl group on the xanthine scaffo...

A one-pot procedure for the synthesis of 5-benzoyl-8H-phthalazino[1,2-b]quinazolin-8-ones is achieved by an iodine-catalyzed reaction of 2-aminobenzohydrazides and 2-alkynylbenzaldehydes in good yields. The salient feature of this strategy is a domino type process including a condensation, addit...

Antimicrobial effects and cytotoxicity of a new quarternaryammonium endodontic antiseptic solution were evaluated and compared with those of sodium hypochlorite and iodine-potassium iodide using in vitro techniques. Iodine-potassium iodide was the least cytotoxic and had the highest antimicrobia...

By means of base-catalyzed ring enlargement of triazaindenoindenes and pentalenoindenes obtained from anhydride-induced ring transformation of 3,4-dihydro-2H-pyrimido- and 2,3-dihydroimidazo[2,1-a]phthalazinium-olates, respectively, a series of pyrazolo[1,5-e]benzo[g][1,5]diazonin-8-ones and pyr...

Starting from 2-aminobenzonitrile 1 and 2-chloromethylbenzoyl chloride 2, a new synthetic pathway to tetracyclic compound 6 is described. Reaction of 2-aminobenzamide 7 with compound 2 leads to the tricyclic ring system 9 which was easily converted to compound 6 in the presence of KOH in refluxi...

We report a large scaled fabrication of AlN nanowires via a chloride-assisted chemical vapor reaction technique at 1100 °C in flowing N2 atmosphere using aluminum powders as starting materials. The as-obtained hexagonal AlN nanowires had the length of hundreds of microns and diameter of 20–100...

During the recent years, selective leaching from laterite ore has gained considerable interest from the scientific community because of the growing demand of valuable metals including nickel and cobalt. However, high energy consumption and serious environmental pollution have been the major draw...