The calcium-sensing receptor antagonist (CaSR) has been recognized as a promising target of anabolic agents for treating osteoporosis. In the course of developing a new drug candidate for osteoporosis, we found tetrahydropyrazolopyrimidine derivative 1 to be an orally active CaSR antagonist that...

Thirty-four newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids were synthesized from 1,2,3,4-tetrafluoro benzene and evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis H37Rv ...

We recently discovered and reported a novel series of benzhydrylpiperazine derivatives bearing an asymmetric carbon atom that are potent and selective hCB1 inverse agonists. In the present study, we used Davis-Ellmann-type sulfonamide chemistry to asymmetrically synthesize two enantiomers of the...

In present work, a complete study of thermodynamic properties of pyruvic acid and methyl pyruvate in the condensed and gaseous phases was carried out using experimental and theoretical approaches. Enthalpies of combustion and formation of compounds were evaluated using combustion calorimetry. Th...

The thermodynamics properties of the mixtures of biodiesel and petroleum-based fuel are useful for the research of blending fuels. Biodiesel is mainly consisting of fatty acid alkyl esters. Densities and viscosity for the binary mixtures of three fatty acid methyl esters (methyl decanoate, methy...

In this study, we compared the performances of three gas chromatography (GC) based microalgal fatty acid methyl esters (FAMEs) analysis methods that are regularly applied to biofuel research using microalgae, specifically the GC-flame ionization detector (GC-FID) with packed and capillary column...

Since elevated osteoclast formation and/or activity by inhibitory responses against pathogens leads to diverse osteolytic bone diseases including periodontitis, inhibition of osteoclast differentiation and bone resorption has been a primary therapeutic strategy. In this study, we investigated th...

1.1. Pantothenate and pantoate inhibit the growth of trypanosoma lewisi in vitro. Salicylate alleviates this inhibition.2.2. Pantothenate, injected into rat, stimulated growth of the trypanosomes early in the infection. There was no detectable effect on ablastin and the immune response. The inhi...

This study has comparatively evaluated the antiradical and antilipid peroxidizing actions of taurine (TAU) and its N-pantoyl analog pantoyltaurine (PTAU) in vitro, and has determined the extent to which these findings agree with the in vivo ability of these compounds to prevent changes in plasma...

A series of 3′-N-acyl-paclitaxel analogues 1a–v were synthesized and their cytotoxicities in vitro against several human tumor cell lines examined. It has been shown that distinct correlation between activity and N-acyl-substituent. The appropriate size of N-acyl group was indispensable for cy...

BackgroundTetranectin is a secreted homotrimeric protein belonging to the C-type lectin family. Our previous studies found that tetranectin was not only related to, but also played a protective role in, Parkinson disease. In this study, we aim to illustrate the molecular mechanism of the secrete...

The alternative ways of synthesis of valuable 5-amino-3-methylisothiazole and 3-methyl-4-nitroisothiazole has been presented and described. It appeared that new, undescribed 3,3′-dimethyl-4,4′-dinitro-5,5′-bisisothiazole has been produced as a side-product during synthesis. Both experimental ...

Knowledge of solubility for 1-methyl-4-nitropyrazole (1-M-4-NP) in different solvents is important for its purification and further theoretical studies. In this paper, the solubility of 1-M-4-NP in toluene, 1,2-dichlorobenzene, water, methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butan...

13C NMR analysis of poly(4-methyl-1,3-pentadiene) (poly(4-MPD)) obtained by using the C2 symmetric zirconocene based catalytic system: rac-[CH2(3-tert-butyl-1-indenyl)2]ZrCl2 (1)/13C enriched methylaluminoxane (MAO) shows strong differences between the microstructure of the first inserted monome...

In order to find a more suitable solvent system, the solubility of 1-methyl-4-nitropyrazole (1-M-4-NP) in three different binary solvents (i.e., water + acetone, water + methanol and water + ethanol) with different mass fraction of water (0.1000, 0.2000, 0.3000, 0.4000, 0.5000, 0.6000 and 0.7000...

[76Br]FBAU is a potential PET tracer for assessing proliferation. This study proposes that [76Br]FBAU 3′,5′-dibenzoate has higher blood-brain-barrier permeability than [76Br]FBAU itself and thus might be better suited for applications in the brain. The brain uptake indexes of the two compounds...

A stereoselective synthesis of 5(S)-12(R) LTB4 is described in this paper using a novel reaction, the sodium amalgam induced reductive elimination of allylic dibenzoates for the selective synthesis of the E,E,Z - triene moiety. The creation of the chiral centers was controled by a chiral sulfoxi...

Introduction1-(2-deoxy-2-[18F]fluoro-β-d-arabinofuranosyl)-5-bromouracil ([18F]FBAU) is a cell proliferation tracer. However, it does not pass readily through the blood-brain barrier. We synthesized a lipophilic prodrug of [18F]FBAU that was intended to enhance brain uptake of [18F]FBAU to impr...

Enzymatic debenzoylation of 1,2-propanediol dibenzoate with 1-octanol has been studied in organic solvent using lipases from different sources. In general a slow, highly regioselective alcoholysis in diisopropyl ether affords exclusively a monoester benzoylated at the secondary hydroxy group alt...

Block copolymers of polypyrrole (PPy) and thienyl end capped cyclohexanone formaldehyde resin (ThCFR) were synthesized via chemical oxidative polymerization of (Py) and ThCFR in the presence of cerium (IV) oxidic dibenzoate (CODB). The treatment of Py with CODB was maintained in non-aqueous medi...