Synthesis, Evaluation and Docking Studies of Disubstituted N-Heterocyclic Derivatives as Anticancer Agents.

Cancer is a chronic disease reported with alarming rates of mortalities every year. Herein, we reported the synthesis of nitrogen based novel heterocyclic disubstituted derivatives and evaluated them against L929 and A549 cell lines using MTT assay. Among all, 6a2 and 6c1 were significantly active against L929 with IC value of 2.

2-Aminoaryl-3,5-diaryl pyrazines: Synthesis, biological evaluation against Mycobacterium tuberculosis and docking studies.

Rationally designed Mycobacterium tuberculosis (Mtb) inhibitors were synthesized under Buchwald conditions using Pd (dba) /xantphos and the compounds were investigated for their biological activity against the Mtb standard strain H37Rv and two other clinically isolated multidrug-resistant strains with different drug resistance patterns. Compounds 5e, 6e, 7e, and 8e exhibited excellent antituberculosis activity against H37Rv with a minimum inhibitory concentration (MIC) value of 15 μg/ml. Compounds 5a, 6c, 7b, 8a, 8b, and 8d also displayed their potency with a MIC value in the range of 15-25 μg/ml.

Enhancement of Loperamide Dissolution Rate by Liquisolid Compact Technique.

The aim of present study was to improve the dissolution rate of poorly soluble drug Loperamide (LPM) by liquisolid compact technique. Liquisolid compacts of LPM were prepared using Propylene glycol (PG) as a solvent, Avicel pH 102 as carrier, Aerosil as coating material and Sodium Starch Glycolate (SSG) as superdisintegrant. Interactions between the drug and excipients were examined by Fourier Transform Infrared (FTIR) spectroscopy.

Development and validation of a stability-indicating RP-HPL C-CAD method for gabapentin and its related impurities in presence of degradation products.

The objective of the current study was to develop and validate a sensitive and specific LC-MS compatible stability indicating reversed phase liquid chromatographic method for the quantitative determination of Gabapentin and its related substances using Corona charged aerosol detection (CAD). The chromatographic conditions were optimized using a Kinetix Biphenyl column with gradient elution using a mobile phase composed of pH 4.2 ammonium acetate, acetonitrile, and methanol.

Phosphodiesterase inhibitor, pentoxifylline enhances anticancer activity of histone deacetylase inhibitor, MS-275 in human breast cancer in vitro and in vivo.

MS-275, a histone deacetylase inhibitor (HDACi), is undergoing clinical trials for treatment of various cancers. Pentoxifylline, a nonselective phosphodiesterase (PDE) inhibitor, has been shown to increase the effectiveness of antitumor chemotherapy. In the present study, the potential anti-cancer activity of MS-275 in combination with pentoxifylline in panel of cell lines and human breast cancer xenograft model were examined.

Hepatoprotective activity of Ficus religiosa leaves against isoniazid+rifampicin and paracetamol induced hepatotoxicity.

Background: The present study was designed to investigate the hepato protective effect of methanolic extract of Ficus religisoa L., Moraceae, on isoniazid-rifampicin and paracetamol induced hepatotoxicity in rats.

Materials And Methods: Male Wistar albino rats were divided into six groups; group 1 served as a control received vehicle (Distilled water), group 2 served as a toxic control, received isoniazid-rifampicin (100 mg/ kg, i.

Bioanalytical method development and validation of memantine in human plasma by high performance liquid chromatography with tandem mass spectrometry: application to bioequivalence study.

A simple, sensitive, and rapid HPLC-MS/MS method was developed and validated for quantitative estimation of memantine in human plasma. Chromatography was performed on Zorbax SB-C(18) (4.6 × 75 mm, 3.