A new oligo(ethylene glycol)-thioacetyl substituted theophylline (THEO) has been synthesized and used to form self-assembled monolayers (SAMs) on different gold substrates. The THEO-SAMs formed are compact and passivate the gold surface in an important extension. The thioacetyl group can be depr...
A series of novel coumarin-theophylline hybrids were synthesized and examined for their anti-tubercular activity in vitro against Mycobacterium tuberculosis H37Rv, anti-microbial activity in vitro against gram-positive bacteria (Staphylococcus aureus) and gram-negative bacterias (Escherichia col...
A new series of theophylline containing acetylene derivatives (6a–6b and 7–13) and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives (20–32) have been designed and synthesized. These compounds were screened for anticancer and antimicrobial activity. Further the compu...
AimsCutaneous melanoma is the most aggressive skin cancer, derived from neoplastic transformation of melanocytes. Since several evidences highlighted the importance of a hierarchical model of differentiation among cancer cells, closely related to resistance mechanisms and tumor relapse, we inves...
The usefulness of azaline B, a GnRH antagonist, in suppressing gonadotropin secretion in the golden hamster was examined by examining follicular development, steroidogenesis and expression of steroidogenic enzymes. Serum levels of P and E declined significantly, while FSH or LH was undetectable ...
Regio- and stereoselective reactions of 2-bromomethyl-1,3-thiaselenole with water and ethylene glycol are accompanied by a rearrangement with the expansion of the five-membered ring to six-membered 2,3-dihydro-1,4-thiaselenine derivatives. The reactions proceed under unusually mild conditions at...
A gas chromatography–mass spectrometric method was developed in this study in order to determine fluoride in plasma and urine after derivatization with 2-(bromomethyl)naphthalene. 2-Fluoronaphthalene was chosen as the internal standard. The derivatization of fluoride was performed in the biolog...
Fluorination of α-bromomethyl aryl ketones using fluorohydrogenate-based ionic liquids as fluorinating reagent is described. Reaction of various α-bromomethyl aryl ketones (1a-g) with fluorohydrogenate-based ionic liquids such as EMIMF·(HF)2.3, PYR13F·(HF)2.3 or PYR14F·(HF)2.3 as a fluoride...
Cyclic voltammograms for reduction of 4-(bromomethyl)-2-oxo-2H-chromen-7-yl acetate (or 7-acetoxy-4-bromomethylcoumarin) (1) at carbon cathodes in either dimethylformamide (DMF) containing tetramethylammonium tetrafluoroborate (TMABF4) or acetonitrile (CH3CN) containing TMABF4 show four irrevers...
A formal [3+3] cyclocondensation of 1,3-bis(silyl enol ethers) with the little-known 4,4-dimethylthio-1,1,1-trifluorobut-3-en-2-one was studied. In contrast to 4,4-dimethoxy-1,1,1-trifluorobut-3-en-2-one, this α-oxoketene dithioacetal reacts with 1,3-bis(trimethylsilyloxy)-1,3-butadienes in the...
Statins inhibit 3-hydroxy-3-methylglutaryl-coenzyme A reductase, which catalyzes the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a rate-limiting step in cholesterol synthesis. Statins are able to reduce cardiovascular risk in hypercholesterolemic patients. In recent years,...
Publisher SummarySimvastatin is a prodrug. After absorption, it undergoes a rapid enzymic hydrolysis of a lactone ring to form the principal metabolite simvastatin β-hydroxy acid. The β-hydroxy acid acts as a potent, reversible, competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (H...
This work investigates an efficient method for purification of simvastatin ammonium salt from the residual amounts of lovastatin ammonium salt. Lovastatin esterase produced by the fungus Clonostachys compactiuscula was chosen as a biocatalyst for selective hydrolysis of lovastatin ammonium salt....
Ten new monoazo disperse dyes (4a–j) have been synthesized by coupling of diazotized 2-amino-4-(2′,4′-dichlorophenyl)-1,3 thiazole (2) with various N-alkyl derivatives of substituted aniline (3a–j) and their dyeing performance on polyester fiber has been assessed. These dyes are characterize...
Some T cell epitopes become inactive when their thiols are blocked with various irreversible reagents (Régnier-Vigouroux, 1988; Maillère, 1992; Maillère et al., 1993). Blocking protein and peptide thiols with BCNP (Boc-Cys(Npys)-OH) constitutes a most appropriate strategy when searching for t...
Background and aimHigh-fat diet (HFD) triggers obesity-related metabolic diseases like non-alcoholic fatty liver diseases (NAFLD). Calcium supplementation is known to have an anti-obesity effect. However, the effect of calcium supplementation has not been evaluated so far in context to hepatic f...
Chia is a good source of calcium, however it is not been previously reported its bioavailability associated with an inflammatory condition. Thus, the present study evaluated the effect of chia on calcium bioavailability, inflammation, and oxidative stress in Wistar rats fed a high-fat diet or st...
Cellular calcium signaling events are transient. Hence they are observed in real time using fluorescence imaging or electrophysiological methods that require sophisticated instrumentation and specialized skills. For high throughput assays simple and inexpensive techniques are desirable. Many cal...
SummaryThe absence of FMR1 protein (FMRP) causes fragile X syndrome (FXS) and disturbed FMRP function is implicated in several forms of human psychopathology. We show that intracellular calcium responses to depolarization are augmented in neural progenitors derived from human induced pluripotent...
ObjectiveIt has been shown that several environmental and physiological factors can affect on the serum levels of calcium and phosphate. The objective of the present study was explored the relationship between serum calcium and phosphate levels with anthropometric and hematological markers.
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