A direct colorimetric assay of zinc in 0.02-ml of serum using a new, water-soluble reagent, 2-(5-nitro-2-pyridylazo)-5-(N-propyl-N-sulfopropylamino)phenol disodium salt dihydrate (nitro-PAPS ϵ = 14.5 × 104 1/mol per cm at 574 nm), is presented. Use of microwell plates allowed a reduction in the...

A regioselective synthesis of both 5-amino- and 3-aminodiarylisoxazoles substituted with polyalkoxyaryl pharmacophores has been validated. Starting materials for the synthetic scheme were easily available from plant extracts. The targeted molecules were further tested in the phenotypic sea urchi...

Enantioselective reductions of 2-X-1-(1,3-benzodioxol-5-yl)-1-ethanones, (X = Cl, Br, N3) by Rhodothorula glutinis CCT 2182 afforded the corresponding (R)-ethanols in good to excellent yields (57–99%) and excellent enantiomeric excesses (>99%). These alcohols may be used as raw materials for th...

The FT-IR and FT-Raman spectra of (E)-1-(1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-one were recorded and analyzed experimentally and theoretically. The observed experimental and theoretical wavenumbers were assigned using potential energy distribution. The NLO properties were evaluated by th...

Seventy nine derivatives of thieno[2,3-b]quinolines, tetrahydrothieno[2,3-b]quinoline, dihydrocyclopenta[b]thieno[3,2-e]pyridine, cyclohepta[b]thieno[3,2-e]pyridine and hexahydrocycloocta[b]thieno[3,2-e]pyridine were either synthesized or obtained commercially and tested for their antiproliferat...

Morphine is widely used for the treatment of severe pain. This analgesic effect is mediated principally by the activation of μ-opioid receptors (MOR). However, prolonged activation of MOR also results in tolerance, dependence, addiction, constipation, nausea, sedation, and respiratory depressio...

New antimicrobial agents, imidazo[1,2-a]pyridine and imidazo[2,1-b][1,3]benzothiazole, have been synthesized. Their antimicrobial activities were conducted against various Gram-positive, Gram-negative bacteria and fungi. Compounds 6c, 7a, 10b, 11a, 12b, 14a, 14b, 15a and 15b, exerted strong inhi...

Aqueous solutions of perfluorinated sulfonic acid (PFSA) ionomers and their side chain model compounds were irradiated with cobalt-60 gamma rays and their reaction products were analyzed by ion chromatography, liquid chromatography with mass spectrometry, and nuclear magnetic resonance spectrosc...

A simple, fast and selective micellar electrokinetic chromatographic (MEKC) method for the simultaneous assay of ketorolac tromethamine and its known related impurities (1-hydroxy analog of ketorolac, 1-keto analog of ketorolac and decarboxylated ketorolac), in both drug substance and coated tab...

Ketorolac tromethamine (KTC) with phenylephrine hydrochloride (PHE) binary mixture (mixture 1) and their ternary mixture with chlorpheniramine maleate (CPM) (mixture 2) were analyzed using a validated HPLC-DAD method. The developed method was suitable for the in vitro as well as quantitative ana...

Study Objective: To determine the efficacy and speed of onset of analgesia of a single dose of intravenous (IV) or intramuscular (IM) ketorolac tromethamine following major orthopedic surgery.Study Design: Double-blind, randomized, placebo-controlled trial.Setting: A district general hospital in...

A method has been developed for the separation of moxifloxacin HCl and ketorolac tromethamine using reverse phase high-performance liquid chromatography (RP-HPLC) on C18 column (250 × 4.6 mm, 5 μm) with UV detection at 308 nm. Experimental designs were applied for multivariate optimization of ...

Polyethylcyanoacrylate (PECA) nanoparticles (NPs) have been employed as biodegradable polymeric carriers for oral (PO) delivery of ketorolac. The nanoparticles were prepared by polymerization technique at room temperature in a continuous aqueous phase at pH 2.5. This polymerization technique was...

Capillary electrochromatography (CEC) was employed for the assay of ketorolac (KT) and its known related impurities [1-hydroxy analog of ketorolac (HK), 1-keto analog of ketorolac (KK), ketorolac decarboxylated (DK)] in both drug substance and coated tablets. Detection was made at 323 nm and flu...

1,7-Dihydrodiimidazo[4,5-b:4′,5′-e]pyridine obtained by reductive heterocyclization was N-arylated with 4-fluoronitrobenzene to form two regioisomers in 7 : 3 ratio. This N-arylation is considered as a model reaction for the polymer synthesis.

Protein kinase C theta (PKCθ) plays a critical role in T cell signaling and has therapeutic potential for T cell-mediated diseases such as transplant rejection and rheumatoid arthritis. Here, a series of 2,4-diamino-5-fluoropyrimidine derivatives were prepared and evaluated for their inhibition...

To obtain a group-specific antibody to 1α,25-dihydroxyvitamin D and its derivatives having the 1α,3β-dihydroxylated A-ring structure, 1α-hydroxy-25,26,27-trinorvitamin D3-24-oic acid was synthesized as a haptenic derivative by a new convenient synthetis route. Three kinds of polyclonal antib...

24-Oxa-vitamin D3 (24-oxa-D3) and 24-oxa-1α-hydroxyvitamin D3 were designed as possible inhibitors of the vitamin D metabolic activation pathway. Their affinity for the vitamin D receptor (from pig intestine) and human vitamin binding protein were reduced, and their potency to induce cell diffe...

Three A-ring analogs of 1α,25-dihydroxyvitamin D3 (1,25(OH)2D3)—2-nor-1,3-seco-1,25(OH)2D3 (2-nor analog), 2-oxa-3-deoxy-25-OH-D3 (2-oxa analog), and A-homo-3-deoxy-3,3-dimethyl-2,4-dioxa-25-OH-D3 (A-homo analog)—were tested for their ability to inhibit 25-OH-D3-1α-hydroxylase (1α-hydroxyla...

Six A-ring analogs of 1α,25-dihydroxyvitamin D3 (1, 1α,25-(OH)2-D3) 3-deoxy-3-thia-1α,25-(OH)2-D3 (3), 3-deoxy-3-thia-1α,25-(OH)2-D3-3α-oxide (6), 3-deoxy-3-thia-1α,25-(OH)2-D3-3β-oxide (7) and the 5,6-trans counterparts 5, 8, and 9, respectively—were tested for their ability to inhibit ...