Five new copper(II)-based ionic liquids and three crystalline compounds have been synthesized in order to further understand the role of the anion in determining their physicochemical properties. Materials were prepared with combinations of three different anions (2-ethylhexanoate (EHN), tetrafl...
A new method for the synthesis of 2-aminomethyl functionalized 1,4-benzodiazepin-5-ones is presented. The benzodiazepine core is well-known to interact with biological receptors and many pharmaceutical drugs are derived from this structure. The alkene diamination strategy is employed for the fir...
Two-armed poly(ɛ-caprolactone) (TAPCL) polymers were successfully synthesized via the ring opening polymerization (ROP) of ɛ-caprolactone (ɛ-CL) using the Schiff's base complexes [Cu(SAEE) 2 ] (1) and [Ni(SAEE) 2 ] (2), which have two hydroxyl functional groups, as the two-site i...
A rapid and sensitive bioassay based on liquid chromatography tandem mass spectrometry (LC–MS/MS) has been developed and validated for the simultaneous determination of eight coumarins in rat plasma. The liquid–liquid extraction method with ethyl acetate was used to prepare the plasma samples ...
In this study, we synthesized several imperatorin analogs using imperatorin and xanthotoxin as substrates. The anti‐cholinesterase activities of all compounds were evaluated in in vitro experiments according to the modified Ellman's method. For each synthesized compound, IC50 values for both en...
Background and Purpose Activation of the human pregnane X receptor (PXR; NR1I2) has potential therapeutic uses for inflammatory bowel disease (IBD). Imperatorin (IMP), a naturally occurring coumarin, is the main bioactive ingredient of Angelica dahurica Radix, which is regularly used to treat th...
Novel agents in combination with melphalan and prednisone (MP) significantly improved progression‐free survival (PFS) and overall survival (OS) in multiple myeloma (MM). Randomized trials comparing MP plus bortezomib (VMP) versus MP plus thalidomide (MPT) are lacking. Nine hundred and fifty‐si...
BackgroundHigh‐dose melphalan (HDM) is an integral component of conditioning regimens for autologous and allogeneic hematopoietic stem cell transplantation for patients with malignant and non‐malignant diseases. The gonadotoxic effects of HDM are often obscured by previous or concurrent admini...
1. Stop injection/infusion immediately 2. Get extravasation kit 3. Put on (sterile) gloves 4. Replace infusion lead or syringe with 5 ml disposable syringe and aspirate slowly as much as possible of the extravasated drug; Cave! do not exert pressure on extravasation area
Benzimidazoles (BZs) remain amongst the most widely used anthelmintic drug classes against gastro-intestinal nematode infections, although their efficacy is increasingly compromised by resistance. The primary underlying mechanisms for BZ resistance are single-nucleotide polymorphisms (SNPs) in t...
In this paper, a simple, rapid and sensitive fluorescence method based on the formation of terbium (Tb3+) complex has been developed for the rapid detection of Tb3+ in water. The fluorescence sensor has been studied by using terbium complexed with thiabendazole (TBZ) while acetonitrile (MeCN) as...
Thiabendazole (TBZH) reacts with iron(III) nitrate causing protonation of the ligand to yield the nitrate salt [TBZH 2 NO 3 ] (1). Reaction of TBZH with copper(II) acetate results in the deprotonation of the ligand yielding [Cu(TBZ) 2 .(H 2 O) 2 ] (2). Rea...
The purpose of this study was to determine the influence of a controlled incremental increase in size, molecular weight and number of amine, carboxylate and hydroxyl surface groups in several series of poly(amidoamine) (PAMAM) dendrimers for controlled ocular drug delivery. The duration of resid...
Poor corneal penetration and short preocular retention of a clinical hydrophilic drug, pilocarpine nitrate (PN), for the treatment of open-angle glaucoma and acute angle-closure glaucoma, limit its ocular application. The purpose of this study was to investigate the potential of liquid crystal n...
The purpose of this paper was to investigate the potential of liquid crystalline (LC) gels for ophthalmic delivery, so as to enhance the bioavailability of pilocarpine nitrate (PN). The gels were prepared by a vortex method using phytantriol and water (in the ratio of 73:27 w/w). Their inner str...
Two new manganese complexes with multidentate 3-methoxysalicylaldehyde benzoylhydrazide ligand have been synthesized and structurally characterized. Variations of the reaction conditions (namely, the base, solvent or the counter ion) lead to drastic changes in the nature of the resulting coordin...
Three organotin(IV) complexes, Ph 2 Sn(mstsc) (1), Me 2 Sn(mstsc) (2) and Bu 2 Sn(mstsc) (3), have been synthesized from reaction of R 2 SnCl 2 (R=Ph, Me and Bu) with 3-methoxysalicylaldehyde thiosemicarbazone (H 2 mstsc). The synthesized complexes...
Two new Schiff base ligands containing 2,4–disubstituted thiazoles and cyclobutane rings, 4-(1-methyl-1-phenylcyclobutane-3-yl)-2-(2-hydroxy-3-methoxybenzylidenehydrazino)thiazole (L1H), 4-(1-methyl-1-p-xylylcyclobutane-3-yl)-2-(2-hydroxy-3-methoxybenzylidenehydrazino)thiazole (L2H) and their m...
The synthesis, thermodynamic and photophysical properties of trivalent metal complexes of biomimetic nonadentate analogue, 5,5′-(2-(((8-hydroxyquinolin-5-yl)methylamino)methyl)-2-methylpropane-1,3-diyl)bis(azanediyl)bis(methylene)diquinolin-8-ol (TAME5OX), have been described. Combination of ab...
Ras converting enzyme 1 (Rce1) is an endoprotease that catalyzes processing of the C-terminus of Ras protein by removing -aaX from the CaaX motif. The activity of Rce1 is crucial for proper localization of Ras to the plasma membrane where it functions. Ras is responsible for transmitting signals...
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