BackgroundThe radiation sterilization is one of the best methods for sterilizing vulnerable degradation drugs like cefozopran hydrochloride.

The isomeric truxillines and their hydrolysis products are present as manufacturing impurities in most illicit, refined cocaine samples. Methodology is described for the comparative gas chromatographic determination of total isomeric truxilline manufacturing impurities/by-products, i.e., intact ...

The thermal exfoliation of pyrophyllite on heating above 600 °C was studied to discern its kinetic pathway and correlate it with dehydroxylation. The irreversible thermal expansion data of pyrophyllite was collected from a thermomechanical analyzer at different heating rates (β). Detailed kine...

The surface charge property and chemical composition are important for flotation investigation. First, the mineral phase and morphology of different pyrophyllite samples were analyzed. The isoelectric points of different pyrophyllite particles also were determined. Moreover, the effect of chemic...

Analysis on suppression effect of depressant on naturally hydrophobic gangue minerals is of great importance for both industrial applications and theoretical research. In this work, the role of glucan in the flotation separation of pyrite and pyrophyllite was studied and the selective depression...

1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (DDPH) is a potent α1-adrenoceptor antagonist that is currently under Phase II clinic trials. However, the fast metabolism has restricted its further use. In this paper, 11 DDPH analogs were designed according to the...

Through a structure-based drug design project (SBDD), potent small molecule inhibitors of pyruvate carboxylase (PC) have been discovered. A series of α-keto acids (7) and α-hydroxycinnamic acids (8) were prepared and evaluated for inhibition of PC in two assays. The two most potent inhibitors ...

N-(2,4-Dimethylphenyl)-2,2-dichloroacetamide (24DMPA) and N-(3,5-dimethylphenyl)-2,2-dichloroacetamide (35DMPA) of the configuration XyC6H5−yNHCOCHCl2 (where, X = CH3 and y = 2) were synthesised and an extensive spectroscopic investigations have been carried out. The ab initio and DFT studies we...

The tautomeric properties of an N-(3,4-dichlorophenyl)-1H-indazole-5-carboxamide (NTZ-1006, 2) derivative, developed as highly potent, reversible and selective MAO-B inhibitor useful for the treatment of Parkinson's disease (PD) and other neurological disorders, have been studied both exper...

Herein, we report synthesis and evaluation of new twenty-eight pyrazinyl ureas against β amyloid (Aβ)-induced opening of mitochondrial permeability transition pore (mPTP) using JC-1 assay which measures the change of mitochondrial membrane potential (ΔΨm). The neuroprotective effect of seven...

The compound 3,4‑dichlorophenyl‑propenoyl‑sec.‑butylamine (3,4‑DCPB) is an antiepileptic drug. The purpose of the present research was to identify cytochrome P450 (CYP450) responsible for the metabolism of 3,4‑DCPB and evaluate the effects of 3,4‑DCPB on the activities of CYP450 enzymes. 3,4‑DCP...

In the present investigation a series of novel 2-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazol-4-yl]-5-(substituted-phenyl)-[1,3,4]oxadiazoles (4a–j) were synthesized by cyclization of substituted-benzoic acid N′-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazole-4-carbonyl]-hydrazide by...

A series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cance...

The beta-thymosins are a family of

Two rabbit polyclonal antisera, one directed against thymosin β4 and the other one against the peptide fragment thymosin β4 (1–14) were characterised by epitope mapping. Hexapeptides representing the whole sequence of the native peptide and overlapping by one amino acid were synthesised on po...

Study the effect of stachydrine hydrochloride to prostatic hyperplasia in mice which made of the urogenital sinus implantation. KM male mices were selected.The group was given the respective drugs for gavage, the group of BG and MG were given the distilled water which the same amount as the drug...

Management of chronic pain is restricted by the lack of effective tools. This study evaluated the efficacies of sinomenine combined gabapentin or ligustrazine hydrochloride in treating peripheral and central chronic neuropathic pain.The study was conducted in mice with photochemically induced sc...

A simple and convenient method has been developed for the preparation of (R)- and (S)-pyrrolidine-2-phosphonic acids. The thermal reaction of proline with diethyl phosphite in the presence of benzaldehyde gave an N-benzyl derivative of diethyl pyrrolidine-2-phosphonate, which was transformed int...

In the present work, two new potentially active quinazolin-4-yl-aminobenzenesulfonamide derivatives, N-(5-methyl-1,2-oxazol-3-yl)-4-[(quinazolin-4-yl)amino]benzene-1-sulfonamide (4a) and N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-[(quinazolin-4-yl)amino]benzene-1-sulfonamide (4b), were synthesized and t...

A series of new 7-monosubstituted and 3,7-disubstituted indazoles have been prepared and evaluated as inhibitors of nitric oxide synthases (NOS). 1H-Indazole-7-carbonitrile (6) was found equipotent to 7-nitro-1H-indazole (1) and demonstrated preference for constitutive NOS over inducible NOS. By...