Journal of Pharmaceutical and Medicinal Chemistry

 A series of 4, 6-diacetyl-1, 3-di(substituted-phenyl carbonyloxy)benzenes or diesters (2a-f) were prepared and screened for in vitro antibacterial and antifungal activities. 1, 1´-(4,6-Dihydroxy-1, 3-phenylene)diethanone (1) was treated with different aromatic acids in dry pyridine in presence of phosphorous oxychloride to obtain the diesters (2a-f). The structures of the synthesized compounds were established on modern analytical techniques. The antimicrobial activity (minimum inhibitory concentration; MIC) of the title compounds was determined against some selected bacterial and fungal strains. The compounds showed appreciable antimicrobial activity against the tested microbes. Presence of halogen group(s) was found to increase the antimicrobial activity of the diesters.

 A simple, rapid, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous estimation of Metformin and Dapagliflozin in tablet dosage form. An Inertsil ODS C18 column having 150 x 4.6mm id in Isocratic mode with mobile phase containing Acetonitrile :  phosphate buffer (70:30 %v/v  pH: 3.0) was used. The flow rate was 1.0ml/min and effluents were monitored at 240nm.) The retention time of Metformin and Dapagliflozin was 2.463min and 3.760min respectively. The concentration curves of Metformin and Dapagliflozin were linear in the concentration range of 50µg/ml-250 µg/ml and 5µg/ml-25µg/ml of Metformin and Dapagliflozin respectively. The developed method was validated for specificity, precision, linearity, accuracy, LOD, LOQ,  robustness. Recovery of Metformin and Dapagliflozin in formulations was found to be in the range of 97.0% -98.0% and 100%-103% respectively confirms the non-interferences of the excipients in the formulation. Due to its simplicity, rapidness and high precision, the proposed HPLC method may be used for the simultaneous determination of these two drugs in pharmaceutical dosage forms. 

 An amide-based mutual prodrug (NA-D) was synthesized by condensing nalidixic acid with dapsone with an aim of preparing a useful drug, which could show broad spectrum of antimicrobial activity. Its structure was established on the basis of elemental analysis, 1H NMR and Mass spectral data results. The mutual prodrug (NA-D) was also evaluated for in-vitro antibacterial and antifungal activity.

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 A series of 1-(2, 4-dimethoxy-5-[3-(substituted-phenyl)acryloyl]phenyl)-4-(substituted-phenyl)but-2-en-1-ones (3a-e) were synthesized and evaluated for their antimicrobial actions. Resorcinol was used as starting material for the preparation of 1, 1´-(4, 6-dihydroxy-1, 3-phenylene) diethanone (1), which then treated with dimethylsulphate to obtain 1-(5-acetyl-2, 4-dimethoxyphenyl)-1-ethanone (2). Compound (2) was reacted with substituted aromatic aldehydes in ethanol in presence of KOH to furnish the title compounds (3a-e). The structures of the synthesized compounds were confirmed on the basis of  1H-NMR, Mass and elemental analysis results. The antimicrobial activity (minimum inhibitory concentration; MIC) of the title compounds was determined against some selected bacterial and fungal strains. Two compounds, 3d and 3e, showed good antimicrobial activity against S. aureus and E. coli.