In this paper, a simple and reproducible method for the determination of roxithromycin in human plasma samples is proposed. The surface magnetic molecularly imprinted polymers (MMIPs) were utilized as sorbent. Roxithromycin was used as imprinted compound. The experimental results showed that the...

Praziquantel has been used for the treatment of diseases caused by infection with various parasites. Praziquantel treatment in Opisthorchis viverrini-infected patients reduces the hepatobiliary fibrosis due to tissue resorption, however, some fibroses are irreversible. To clarify the effect of p...

Isolated rat hepatocytes were used to elucidate the metabolism of praziquantel (PZQ). Our studies were designed to investigate mainly qualitative differences in the biotransformation of PZQ enantiomers. Additionally, the main metabolites cis- and trans-4-hydroxypraziquantel were determined semiq...

Praziquantel (PZQ), prescribed as a racemic mixture, is the most readily available drug to treat schistosomiasis. In the present study, ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC–ESI-QTOFMS) based metabolomics w...

A new method for the synthesis of praziquantel enantiomers via resolution of praziquanamine with (S)-(+)-naproxen was developed. The four 4′-hydroxy derivatives were obtained through each single praziquanamine enantiomer, coupling with cis- and trans-4-(benzyloxy)cyclohexanecarboxylic acids and...

Spinal muscular atrophy (SMA) is a neurodegenerative disease caused by loss of survival motor neuron-1 (SMN1). A nearly identical copy gene, SMN2, is present in all SMA patients. Although the SMN2 coding sequence has the potential to produce full-length SMN, nearly 90% of SMN2-derived transcript...

New and efficient methods for the synthesis of N1-substituted and C6-substitued adenines were developed from the easily accessible 5-aminoimidazole-4-carboxamidines. Condensation of these compounds with triethyl orthoformate led to the selective synthesis of the N1-substituted adenines. Regiosel...

Thrombus formation presents a serious hindrance in the development of functional artificial blood vessels, especially those with a small diameter. Endothelialization can prevent thrombus formation; however, the adhesion of endothelial cells to existing polymer materials is generally weak. Theref...

In this study a new monospirocyclic phosphazene derivative, 4′,4′,6′,6′-tetrachloro-3-(2-methoxyethyl)-3H,4H-spiro [1,3,2-benzoxazaphosphinine-2,2′- [1,3,5,2,4,6] triazatriphosphinine] (SP1) was synthesized from the reaction of hexachlorocyclotriphosphazene (N3P3Cl6) with N/O donor-type, 2-...

We have used single-crystal X-ray structural analysis and Raman spectroscopy to study the crystalline structure and conformational properties of a quaternary ammonium ionic liquid, N,N-diethyl-N-methyl-N-(2-methoxyethyl) ammonium iodide ([DEME][I]). At 296 K the crystal structure of [DEME][I] wa...

3-[(2H-1,2,4-Benzothiadiazine-1,1-dioxide-3-yl)thio]-2-methylpropanoic acids were synthesized from the corresponding 3-mercaptoderivatives by alkylation with (+) (R)- and (−) (S)-3-bromo-2-methylpropanoic acid methyl ester. The nucleophilic substitution takes place with complete maintenance of t...

Asymmetric synthesis of 3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxides (DHBDs) was realized using readily available scandium(III)-inda-Pybox as the catalyst. It represents the first example focusing on systematic study of asymmetric synthesis of DHBDs, and a series of enantioselective 3-alky...

Condensations of o-halo-substituted benzenesulfonyl chlorides with 2-aminopyridines and amidines may give the corresponding 1,2,4-benzothiadiazine-1,1-dioxides under mild, non-catalytic conditions in nearly quantitative yields. The successful one-pot cyclization depends on three factors: (i) the...

Analytical high-performance liquid chromatography (HPLC) methods using derivatized cellulose chiral stationary phases (CSPs) were developed for the separation of the enantiomers of 7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide ((±) IDRA21). In previous studies, (±) IDRA21...

A novel stopped-flow multidimensional HPLC (sf-MD-HPLC) procedure has been developed to investigate simultaneously the effect of the pH on the enantiostability and hydrolysis of (±)-7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide [(±)IDRA21]. It was possible to determinate ...

Two novel perfluorodiarylethenes which contains a 2-methylbenzo[b]furane and a modified pyridine moiety were synthesized. Such structure may induce F⋯N or S⋯N heteroatom contact which was newly observed. Experiments results showed that the photocyclization quantum yield exhibited a strong correl...

Ethyl (tributylstannyl)acetate adds chemoselectively to acylpyridinium salts to yield a variety of dihydropyridines with diverse functional groups. These compounds are useful precursors for the preparation of a variety of N-heterocycles. The regiochemistry of the reaction is addressed and the re...

A series of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides (IPAs), based on the structure of WZY02 discovered in our lab, were designed and synthesized as new anti-TB agents. Results reveal that many of them exhibit excellent in vitro inhibitory activity with low nanomolar MIC values a...

Some reports indicate that the silver released from dermally applied products containing silver nanoparticles (AgNP) (e.g. wound dressings or cosmetics) can penetrate the skin, particularly if damaged. AgNP were also shown to have cytotoxic and genotoxic activity. In the present study percutaneo...

Zirconium compounds have been associated with the development of hypersensitivity granulomas. However, aluminum zirconium complexes have not previously been shown to induce sensitization. We present the clinical and histologic findings of a case in which a patient developed an acute hypersensiti...