Synthesis of novel heterocyclic Quinolone compound for anti -tubercular activity

In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen quinolone nucleus for study and over it. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance. Methodology: The synthesis of Quinolone derivatives, starting from substituted aniline and ethyl acetoacetate, by conventional organic reaction and results of investigations of their anti-mycobacterial activity. Results: MICs of the synthesized compounds are compared with existing drugs Cytotoxicity. The substituted quinolones are synthesized by taking mixture of 7-substituted-2-(3-chloro-2-oxopropyl) quinolin-4(1H)-one and different secondary amines. Many compounds have shown promising activity while some were inactive. Conclusion: It was found that Compound A1, A3, B1, B3, have shown promising anti tubercular activity whereas compound A2, A4, B2, B4 were showing moderate anti tubercular activity against std. Streptomycin

Synthesis of novel heterocyclic Quinolone compound for anti -tubercular activity

In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen quinolone nucleus for study and over it. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance. Methodology: The synthesis of Quinolone derivatives, starting from substituted aniline and ethyl acetoacetate, by conventional organic reaction and results of investigations of their anti-mycobacterial activity. Results: MICs of the synthesized compounds are compared with existing drugs Cytotoxicity. The substituted quinolones are synthesized by taking mixture of 7-substituted-2-(3-chloro-2-oxopropyl) quinolin-4(1H)-one and different secondary amines. Many compounds have shown promising activity while some were inactive. Conclusion: It was found that Compound A1, A3, B1, B3, have shown promising anti tubercular activity whereas compound A2, A4, B2, B4 were showing moderate anti tubercular activity against std. Streptomycin

SYNTHESIS OF COUMARIN HETEROCYCLIC DERIVATIVES WITH IN-VITRO ANTITUBERCULER ACTIVITY

In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen coumarin nucleus for study. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance. The synthesis of coumarin derivatives, starting from salicyaldehyde and ethyl acetoacetate, by conventional organic reaction and results of investigations of their anti-mycobacterial activity. MICs of the synthesized compounds are compared with existing drugs Cytotoxicity. Many compounds have shown promising activity while some were inactive. It was found that Compound A1, A2, B1, B2, C1, C2 have shown promising antitubercular activity against std. Streptomycin  Keywords: Coumarin derivative, well diffusion method, antitubercular activity

Development and Validation of Analytical Method for Simultaneous Estimation of Formoterol Fumarate Dihydrate and Fluticasone Propionate from Bulk and Dry Powder Inhaler Formulation

A method was developed and validated for analysis of Formoterol Fumarate and Fluticasone Propionate in dry powder inhaler formulations. Separation was achieved on a HiQ Sil C18HS, 250×4.6 mm, 5 µm column using a mobile phase consisting of Acetonitrile: 0.01 M Ammonium Dihydrogen Phosphate solution (80:20 %v/v) at a flow rate of 1ml/min PDA detection at 215.0 nm. This method is validated according to ICH guidelines, which include linearity, precision, accuracy, specificity, robustness. The result obtained were within the acceptance criteria as per ICH guidelines. Keywords: formoterol fumarate dihydrate, fluticasone propionate, buffer, HPLC

A Review on Development and Validation of Analytical Method for Simultaneous Estimation of Formoterol Fumarate Dehydrate and Fluticasone Propionate from Bulk and Dry Powder Inhaler Formulation

To compare the effectiveness of formoterol fumarate dihydrate and fluticasone propionate two combination inhaled corticosteroid/long acting beta–agonist product approved for treatment of chronic obstructive pulmonary disease (COPD) in the US with respect to cost, therapy adherence, and related healthcare utilization. UV– method for formoterol fumarate dihydrate (FFD) and fluticasone propionate (FP) is simultaneous equation method, Absorbance ration method, first order derivative method the wavelength of FFD-236nm, FP-215nm, overlay of FFD and FP is 233nm. The process can be used for routine simultaneous analysis of formoterol fumarate dihydrate and fluticasone propionate in dry powder inhalation formulation. Early dry powder inhalers (DPIs) wear designed for low drug doses in asthma and COPD therapy. This study contains carrier- based formulations and lacked efficient dispersion principles. Therefore, partial engineering and powder processing are increasingly applied to achieve acceptable lung deposition with this poorly designed inhaler

A Rapid and Sensitive stability indicating Rp-HPLC method development for the quantitative analysis of empagliflozin & linagliptin in bulk & synthetic mixture

An isocratic HPLC method was developed using, Shimadzu C18 column (250 mm × 4.6 mm, 5 µm) with an isocratic binary mobile phase consisting of Acetonitrile: Buffer in a ratio (80:20 v/v) pH 3.0 adjusted with Orthophosphoric acid and flow rate monitored at 0.80 ml/min. The UV detector was used for simultaneous analysis of two drugs at a common wavelength of 226 nm and each injection volume was 20 µl. The retention time for Empagliflozin and Linagliptin was found to be 3.714 min and 3.064 min, respectively. Empagliflozin and Linagliptin produce degradation products in acidic, alkaline, thermal, and UV stress. The result of the assay of Empagliflozin and Linagliptin shows that the degradation product does not interfere with the analytical procedure quantitively when these drugs are analyzed

Development and Validation of Analytical Method for Simultaneous Estimation of Formoterol Fumarate Dihydrate and Fluticasone Propionate from Bulk and Dry Powder Inhaler Formulation

A method was developed and validated for analysis of Formoterol Fumarate and Fluticasone Propionate in dry powder inhaler formulations. Separation was achieved on a HiQ Sil C18HS, 250×4.6mm, 5µm column using a mobile phase consisting of Acetonitrile: 0.01 M Ammonium Dihydrogen Phosphate solution (80:20 %v/v) at a flow rate of 1ml/min PDA detection at 215.0 nm. This method is validated according to ICH guidelines, which include linearity, precision, accuracy, specificity, robustness. The result obtained were within the acceptance criteria as per ICH guidelines