Pramila T

In pharmaceutical products the presence of impurity assures the quality. It is important to identify potential source of impurities. Estimation of impurities is done by variety of chromatographic and spectroscopic techniques either alone or combination with other techniques. These different methods for detecting and characterizing impurities with IR, TLC, HPLC, MASS, NMR, HPTLC etc.  

Several pharmacological activities like antitubercular, analgesic, anti-cancer, anti-inflammatory, antiasthmatic, antioxidant and antibacterial activities have been attributed to pyrazoles. The above observations prompted us to synthesize some novel pyrazole derivatives as possible antimicrobial agents. A series of novel 1,3,5-trisubstituted pyrazole derivatives (P1-P15) have been synthesized by the reaction of substituted chalcones (C1-C15) with succinichydrazide. The starting material, chalcones were prepared by claisen Schmidt condensation of acetophenone with aldehydes in the presence of sodium hydroxide in ethanol. Succinichydrazide was synthesized by condensing succinic acid with hydrazine hydrate. The cycloaddition of chalcones with succinichydrazide gives 1,3,5-trisubstituted pyrazole derivatives. The structures of synthesized derivatives were confirmed by IR, 1HNMR and Mass spectrum. The synthesized compounds were screened for their antibacterial and antifungal activity. The antibacterial activity data of the synthesized derivatives revealed that the compound P4, P13 and P7, P14 were effective against gram positive and gram negative organisms respectively. The antifungal activity data revealed that the compound P7 and P8 showed good activity against tested fungi.

Several pharmacological activities like anti-cancer, anti-microbial, antibacterial, antifungal, and anti-viral activity have been attributed to tetrahydrocarbazole. The above observations prompted us to synthesize some novel tetrahydrocarbazole derivatives as possible anticancer agents. A series of novel tetrahydrocarbazole derivatives have been synthesized by the reaction of tetrahydrocarbazole with substituted aromatic aldehydes. The starting material, tetrahydrocarbazole were prepared by Fischer indolisation reaction of cyclohexanone with phenylhydrazine in the presence of acetic acid. The cycloaddition of tetrahydrocarcazole and substituted aromatic aldehydes gives tetrahydrocarbazole derivatives (A1-A10). The structures of synthesized derivatives were confirmed by IR, 1HNMR and Mass spectrum. The synthesized compounds were screened for their in-vitro anticancer activity. The anticancer activity data of the synthesized derivatives were found to be potent activity. Key words: Phenyl hydrazine, Cyclohexanone, Tetrahydrocarbazole derivatives, In-vitro anticancer activity.

In the present scheme, we have an attempt to synthesize some novel benzimidazole derivatives by substituting triazole moiety at N-1 position of benzimidazole by fusion reaction of benzimidazole-1-acetic acid with thiocarbohydrazide. The substituted triazole was refluxed with different aromatic carboxylic acid in the presence of POCl3 yield different benzimidazole derivatives, respectively. The synthesized compounds were characterized by IR, 1H-NMR and Mass spectroscopy. The compounds were screened for antibacterial (gram +ve, gram –ve bacteria) activities. Key words: Benzimidazole, thiocarbohydrazide, substituted benzoic acid, benzimidazole- 1-acetic acid

  A new, simple, economic and sensitive UV-spectrophotometric method was developed for the determination of Sorafenib in bulk and pharmaceutical formulations. The developed spectrometric method was validated for selectivity, linearity, range, precision, accuracy, ruggedness and sensitivity. The method has demonstrated excellent linearity over the range of 2-10 μg/ml with regression equation: y=0.079x-0.0081 and regression correlation coefficient r2=0.999. The developed method demonstrated consistent high recoveries (97–99%) and low relative standard deviation (< 5%) at 265 nm. Moreover, the method was found to be highly sensitive with low limit of detection (0.028 μg/ml) and limit of quantitation (0.085 μg/ml). The apparent molar absorptivity and Sandell's sensitivity was found to be 48.09 mol-1cm-1 and 0.013245 µg/cm2, respectively. The validated method was successfully employed for the drug content analysis from tablet preparations. Additionally, the method was also employed for pH metric solubility analysis of the drug.