Objective: A simple, selective, sensitive, specific, and spectrophotometric method has been developed for the detection of imatinib mesylate in pure form and formulations. Methods: The analytical condition was optimized for the drug, carried out as per the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use guidelines. Results: The drug shows absorption at 232.0 nm and obeyed beers law in the wide concentration range from 0.5 to 4.0 μg/ml. The lower limit of detection was found to be 0.331 μg/ml and the limit of quantification to be 1.004 μg/ml. The regression equation was found to be y = 0.08x. The precision of the method was found to be 99.04%±0.527% and the percentage of drug recovered by this method is 100.13%±1.375%. Conclusion: The method is simple and suitable for determination for imatinib mesylate in pure and pharmaceutical preparation.

This study was designed to evaluate the toxicity of the n-butanol extract of marine derived fungi Aspergillus protuberus sp1. Lethal dose (LD50), chronic and sub acute toxicities were determined in the rats. From the LD50, the effective dose (ED50) was determined. The n-butanol extract was prepared at the concentrations of 200, 400, and 600 mg.kg -1 body weight. In the sub acute toxicity study, the prepared extract was given orally to the experimental rats for fourteen days and in case of chronic toxicity study, it was given for ninety days. Then the animals were observed for the biochemical and hematological effects, macroscopic and microscopic changes in the liver and kidney. Results showed that, in both sub acute and chronic toxicity studies, the experimental rats showed normal general behavior, respiratory pattern, cardiovascular signs, motor activities, reflexes and normal change in skin and fur. The results also showed that the extract did not induce any biochemical, hematological effects, macroscopic and microscopic changes in the liver and kidney. Collectively, these data demonstrate that the extract is safe and these results are useful for further investigation of this fungus in the future.

Objective: The present study was aimed to design and evaluate the antidiabetic potential of novel 2-aminobenzimidazole derivatives by in silico method. Materials and Methods: Various in silico tools such as Chemsketch, Molinspiration, Prediction of activity spectra for substances, OpenBabel, Discovery Studio was used in the designing and evaluation of the biological activity. The retrieved hits were further filtered by absorption, distribution, metabolism, and excretion descriptors. The designed molecules having required physicochemical properties, drug-likeness, and obeying Lipinski’s rule of five were selected for the synthesis. The synthesized compounds were subjected to determination of yield, melting point and characterized by infrared, 1HNMR, 13CNMR, and mass spectroscopic methods. The selected derivatives were subjected to in vitro glucose uptake, 50% lethal dose (LD50) determination, gene expression analysis, and α-glucosidase inhibitory assay. Results: Totally, 32 novel analogs of 2-aminobenzimidazole were designed and 17 compounds were selected for docking analysis; and finally, five derivatives (3a, 3c, 3e, 3f, and 3h) were selected for synthesis. Among them, the compounds 3a and 3f were selected for in vitro glucose uptake analysis. Finally, the compound 3f was selected for LD50 determination, gene expression analysis, and α-glucosidase inhibitory assay. The selected derivative 3f showed a significant α-glucosidase inhibitory activity compared with the standard drug acarbose. Conclusion: These results are useful for further investigation in the future, and hopefully, these studies could discover a new specific leads in antidiabetic category as α-glucosidase inhibitor.