ISSN : 0970 - 020X, ONLINE ISSN : 2231-5039
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Abstract

Synthesis, Characterization and Biological Activity of Novel Salt/Molecular Salts of Tinidazole

Rama Chandra Murthy Patnala1,2, Mukkanti Khagga2, Ram Bhavani 3 and Vasudha Bhavani4

DOI : http://dx.doi.org/10.13005/ojc/330235


Abstract:

The present study is the continuation of our recently published work on novel salts of Tinidazole, in this study, new solid forms i.e salt/molecular salts of Tinidazole with certain selected organic acids such as hydroxyl benzoic acids, oxalic acid and para-toulenesulphonic acid (TN-organic acids) and inorganic acid such as hydrochloric acid (TN-HCl) were prepared and tested for the solubility parameter. The solubility of TN (compound 1) is 3.7 mg /mL, TN-HCl (compound 2) is 321.2 mg/mL and TN-PTSA (compound 3) is 184.2 mg /mL. These results clearly indicates enhancement of solubility by 86.8 folds and 49.7 folds respectively when compared to TN. These new solid phases (compounds 1-11) were characterized by IR, 1H NMR and DSC and were evaluated for various biological activities viz., anti-antibacterial, analgesic and anti-inflammatory activity. Compounds, TN-PTSA and TN-EBA exhibited good antibacterial activity against the Gram negative bacterial strain, Bacillus subtilus. In case of anti-inflammatory activity studies, TN-PTSA,TN-HCl,TN-DBA exhibited significant activity ranging from 45 to 50 % when compared to TN (50.7%) but exhibited moderate activity in comparison to the standard drug Diclofenac sodium (67.3%).  While, in case of analgesic activity, TN-PBA, TN-PTSA, TN-VA exhibited prominent activity ranging from 78 to 86 % when compared to TN (94.1%) but exhibited moderate analgesic activity in comparison to the standard drug morphine (97.3%).

Keywords:

Salts; Molecular salts; Tinidazole; Hydroxybenzoic acid; Anti-inflammatory activity; Analgesic activity; Solubility

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