A series of novel 7-(4-alkoxyimino-3-amino-3-methylpiperidin-1-yl)fluoroquinolone derivatives were designed, synthesized and characterized by 1H NMR, MS and HRMS. These fluoroquinolones were evaluated for in vitro antibacterial activity against representative Gram-positive and Gram-negative stra...

In this study, we evaluated the insulin-sensitizing effect of flavans purified from Broussonetia kazinoki Siebold (BK) on 3T3-L1 adipocytes. Among the tested compounds, kazinol B enhanced intracellular lipid accumulation, gene expression of proliferator-activated receptorγ (PPARγ) and CCAAT/en...

A sensitive and selective differential pulse-adsorptive anodic stripping voltammetry (DP ASV) method has been developed for trace determination of timolol maleate drug in complex matrices. The established method is first of its kind for timolol maleate (TM) determination with a wide linear dynam...

Despite exponential growth in research relating to sustained and controlled ocular drug delivery, anatomical and chemical barriers of the eye still pose formulation challenges. Nanotechnology integration into the pharmaceutical industry has aided efforts in potential ocular drug device developme...

Despite frequent scientific efforts, efficient ocular drug delivery is a major challenge for pharmaceutical scientists. Poor bioavailability of ophthalmic solutions can be overcome by using smart ophthalmic drug-delivery systems. In this research, loading and delivery of Timolol Maleate (TM) thr...

Advances in nanotechnology have enabled solutions for challenging drug delivery targets. While the eye presents numerous emerging opportunities for delivery, analysis and sensing; issues persist for conventional applications. This includes liquid phase formulation localisation on the ocular surf...

Glaucoma treatment with ocular medications requires overcoming the corneal barrier to drug penetration. Liposomes have a great corneal penetration ability and affinity while suffering from poor stability and low entrapment of hydrophilic drugs accompanied by rapid drug release. This work aims to...

An enantioselective supercritical fluid chromatography (SFC) method was developed and validated to meet the current European Pharmacopoeia requirements of a limit test for the determination of S-timolol maleate enantiomeric purity in timolol maleate drug substance. The developed method is presen...

Supercritical CO2 impregnation was applied to loading of vitamin E into silicone hydrogel for development of controlled release system of timolol maleate, hydrophilic ocular drug for glaucoma. Vitamin E was loaded into the silicone hydrogel to reduce the diffusivity of timolol maleate. Supercrit...

In the present investigation, the effect of timolol maleate loaded ocuserts was studied as an alternative for conventional anti-glaucoma formulation. Ocuserts were prepared using natural polymer sodium alginate and ethyl cellulose. Physico-chemical properties along with drug entrapment efficienc...

A series of N-alkylmaleimides was shown to inactivate effectively the rat liver glucocorticoid receptor at neutral pH. A partial purification of the unbound cytosolic receptor by protamine sulfate precipitation and a careful stabilization of the essential thiol by dithiothreitol and sodium molyb...

A novel (2E)-3-(2,6-dichlorophenyl)-1-(3,4-dimethoxyphenyl)prop-2-en-1-one (DCPDMP) compound has been synthesized and its single crystal has been grown by slow evaporation technique. The structure of the compound has been characterized by FT-IR, FT-Raman and single-crystal X-ray diffraction tech...

In the present study, the spectroscopic characterization of a novel thiazole scaffold was studied. The formation of title compound 4-(2,4-dichlorophenyl)-N-(2,6-dichlorophenyl)-1,3-thiazol-2-amine(6) was evidenced through the changes in FTIR, 1H NMR, LCMS Data. The X-ray diffraction studies reve...

Water structures of hydrated polymers have been suggested to directly influence the biomolecules’ adsorption. We conducted a serial of molecular dynamics simulations to investigate the water structures of hydrated poly(2-methoxyethyl acrylate) (PMEA). According to the calculated IR spectra of w...

The solubilities of CO2 in 2-methoxyethyl acetate, 1-methoxy-2-propyl acetate, and 3-methoxybutyl acetate were measured by isothermal synthesis method under pressures up to 1.2 MPa and at temperatures ranging from (293.15 to 333.15) K. Henry’s constant was calculated based on experimental data ...

The IL (ionic liquid) 1-(2-methoxyethyl)-3-methylimidazolium bis[(trifluoromethyl)sulfonyl]imide [MOEMIM][NTf2] was prepared and confirmed by 1H NMR (1H nuclear magnetic resonance) spectroscopy and 13C NMR (13C nuclear magnetic resonance) spectroscopy. The density and surface tension for the bin...

Novel one-pot reaction conditions have been developed for the preparation of glycosyl thiourea derivatives directly from glycosyl azides mediated by a combination of sulfamic acid and sodium iodide. The reaction conditions were clean, non-toxic and the products were isolated in good to excellent...

The 3,4-dimethoxybenzyl group was used to N-protect 3,4-diphenyl 1,2-thiazetidine 1,1-dioxide derivatives. It is smoothly eliminated by 2,3-dichloro 5,6-dicyanobenzoquinone (DDQ), the yield depending on the substituents of the 3-phenyl ring.

Iron tetrasulfophthalocyanine (FePcTs) catalyzes oxidation of 3,4-dimethoxybenzyl alcohol (DMBA) to ≤ 11% 3,4-dimethoxybenzaldehyde (DMBAL), ≤ 7% 2-hydroxymethyl-5-methoxy-1,4-benzoquinone (HMBQ) and other unidentified products in aqueous hydrogen peroxide at 30–40°C. The FePcTs is unstable ...

Small conductance Ca2+-activated K+ (SKCa) channels play an important role in many functions such as neuronal communication and behavioral plasticity, secretion, and cell proliferation. SKCa channel modulation is associated with various brain, heart, and cancer diseases. N-methyl-laudanosine and...