International Journal of Pharmaceutical Sciences and Drug Research

88-95

Authors: Reena Singh, Nitin Kumar, Mithlesh Yadav, Devender Pathak*

Benzodiazepines and their derivatives were reported to have wide biological activities and were synthesized by the reaction between substituted benzaldehydes and substituted ketones in presence of sodium hydroxide to afford chalcones and further reaction between 1, 2-diamine under smooth condensation with chalcones in presence of glacial acetic acid afforded a new class of 1, 5-benzodiazepines in good yield. 2, 4-disubstituted 1, 5-benzodiazepine derivatives (1B-19B) were synthesized by microwave and conventional methods. The synthesized compounds were evaluated for their antibacterial, antifungal, anthelmintic and cytotoxic activity. The chemical structures of the newly synthesized compounds have been confirmed by IR, 1H-NMR, MASS spectral data and elemental analysis. All the synthesized substituted benzodiazepines have shown good antimicrobial activity, moderate to good anthelmintic activity and possessed significant cytotoxic activity.

101-104

Authors: Jennifer Fernandes, Pankaj Kumar*, Abhishek Kumar

In order to develop relatively small molecules as pharmacologically active molecules, a series of novel oxazolidinones having benzothiazinen and their derivatives were synthesized, and characterized by IR, 1H NMR and Mass spectral studies. Various substituted oxazolidinones benzothiazinen were prepared by simple reflux in the presence of acetonitrile. Treatment of these oxazolidinones benzothiazinen derivatives with methanesulfonyl gives its sulphonates derivatives on further treatment with sodium azide and tri phenyl phosphine in acetic anhydride to give its acetamide derivatives. Further the synthesized compounds were evaluated for antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and antifungal activity against, Candida albicans and Aspergillus niger. The synthesized compounds were screened for their anti-inflammatory activity by carrageenan induced paw-edema method.

108-112

Authors: A. E. Irondi1*, K. K. Anokam2, P. C. Chukwuma3

Variation in the in-vitro antioxidant properties and α-amylase inhibitory activity of Tetrapleura tetraptera pod was assessed at two phenologic stages of the fruit development, that is, the mature green (MG) and ripe brown (RB) stages. RB pod (RBP) had significantly higher (P < 0.05) antioxidant phenolic phytochemicals - total phenol, tannin and total flavonoid - levels than the MG pod (MGP). Conversely, MGP had significantly higher (P < 0.05) total carotenoid and vitamin C contents than RBP. Methanolic extracts of both MGP and RBP had appreciable trolox equivalent antioxidant capacity (TEAC), and were effective in reducing Fe3+ to Fe2+. However, RBP extract had significantly higher (P < 0.05) TEAC and ferric reducing antioxidant power (FRAP) than MGP extract. Furthermore, both MGP and RBP extracts scavenged 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical in a dose-dependent manner, with the half maximal inhibitory concentration (IC50) of RBP (0.11 mg/ml) being lower than that of MGP (0.16 mg/ml). Both extracts also displayed potent inhibitory activity against porcine pancreatic α-amylase in a dose-dependent manner, having IC50 values of 0.33 mg/ml and 0.46 mg/ml for RBP and MGP respectively. Therefore, T. tetraptera pod is more potent in scavenging free radicals and inhibiting pancreatic α-amylase in vitro when fully ripe than when green, and thus could be more effective in alleviating oxidative stress and managing postprandial hyperglycemia in type 2 diabetes at the fully ripe stage than at the mature green stage.

120-124

Authors: Lalit Singh Ranawat1∗, Jagruti Patel2

The scientific evaluation of medicinal plants used in the preparation of folk remedies has provided modern medicine with effective pharmaceuticals for the treatment of diseases. The ethanolic extract of Zanthoxylum armatum DC bark was investigated for its hepatoprotective and antioxidant effects on Paracetamol (500 mg/kg) induced acute liver damage in Wistar albino rats. Hepatoprotection activity was measured by using biochemical parameters such as serum glutamate oxalate transaminase and se-rum Glutamate Pyruvate Transaminase (SGOT and SGPT), alkaline phosphatase (ALP), bilirubin and total protein. The ethanolic extract of Zanthoxylum armatum DC(EZA) at the doses of (100 mg/kg ,200 mg/Kg and 400 mg/Kg) produced significant hepatoprotective effect by decreasing the activity of serum enzymes, bilirubin and lipid peroxidation while it significantly increased the levels of glutathione (GSH), catalyse (CAT) and super oxide dismutase (SOD) in a dose dependant manner. The effects of EZA were comparable to that of standard drug silymarin. These results suggest that EZA may have potential therapeutic value in the treatment of some liver disorders, probably by its antioxidative effect on hepatocytes.

129-132

Authors: Mohd Tariq1*, Shahid S Chaudhary1, Roohi Zaman1, Khaleequr Rahman1, Shaikh Imtiyaz2

Abrak (Mica) is a rock forming silicate of aluminium and is used in Unani system in the form of kushta (calcined product). After proper purification and incineration abrak becomes highly potent and is used in treatment of various diseases of respiratory system, stomach and intestine, tuberculosis, asthma, spermatorrhoea etc. Hakim describes abrak as antipyretic, general tonic, aphrodisiac, constipative and desiccant. Product standardization of a compound formulation is utmost necessary to check the purity and genuineness of a preparation. In this study the purification, preparation and standardization of kushta abrak safaid was performed. Kushta was evaluated on classical parameters like finger test, fineness test etc. as well as on modern parameters like bulk density, tapped density, hausner’s ratio, carr’s index, pH, loss of weight on drying, total ash, acid insoluble ash, water soluble ash, extractive value and loss of weight on ignition. The physicochemical parameters evaluated in this study might be considered as standard parameters of kushta abrak safaid.