In the present work, some new imidazole derivatives (3i-xii) were synthesized as per design synthetic protocol scheme. The structures of newly prepared compounds were confirmed by modern analytical technique (IR, 1H-NMR, Mass spectral data) and elemental analysis, results found in full agreement with their assigned structures. All the synthetic compounds were screened for their antimicrobial activity against bacterial strains viz. Escherichia coli (E. coli, MTCC 2961), Staphylococcus aureus (S. aureus, MTCC 3160), Bacillus subtilis (B. subtilis, MTCC 121), Klebsiella pneumoniae (K. pneumoniae, MTCC 3040) and Micrococcus luteus (M. luteus, MTCC 7527)) and fungal strains viz. Candida albicans (C. albicans, MTCC 227), Aspergillus niger (A. niger, MTCC 277) and Aspergillus flavus (A. flavus, MTCC 418) ; results showed good to remarkable activity. The MIC (minimum inhibitory concentration) values were determined by comparison to ciprofloxacin (anti-bacterial) and fluconazole (anti-fungal) as standard drug. Among them, compound 3iv and 3x exhibited notable antimicrobial activity. These compounds may be used as new template for the searching of potential antimicrobial agents.
Granulation is a size enlargement process, in fine or coarse particles converted into physically stronger and larger agglomerates having good flow property, better compression characteristics and uniformity, prevent segregation of the blend components, improve content uniformity, and eliminate excessive amounts of fine particles. Size of granules has a size range of 0.2 to 4.0 mm, depending on their subsequent use. Size of the granules depends on the quantity and feeding rate of granulating liquid. The selection of process to prepare granules requires thorough knowledge of physicochemical properties of the drug, excipients, required flow and release properties, to name a few. At current scenario available technologies includes, spray drying, roller compaction, high shear mixing, and fluid bed granulation etc. The objective of present work is to focus on the commonly used and novel granulation technologies like such as pneumatic dry granulation, steam granulation, moisture-activated dry granulation, thermal adhesion granulation, freeze granulation, and foamed binder or foam granulation.
Objective: Some new imidazole derivatives (3i-xii) were synthesized as per design synthetic protocol scheme. The structures of newly prepared compounds were confirmed by modern analytical technique and elemental analysis. Methods: All the synthetic compounds were screened for their antimicrobial activity against bacterial results showed good to remarkable activity. The MIC (minimum inhibitory concentration) values were determined by comparison to ciprofloxacin (antibacterial) and fluconazole (anti-fungal) as standard drug. Among them, compound 3iv and 3x exhibited notable antimicrobial activity. These compounds may be used as new template for the searching of potential antimicrobial agents. Results: The purity of the compound was verified with the help of TLC (B: A, 9:1). % age of yield was found 83% and melting point noted 151-1520C. Compounds (3ii, 3viii and 3ix) were shown moderate activity against E. coli, S. aureus, M. luteus and K. pneumonia, whereas compounds (3iii, 3vii, 3xi and 3xii) showed mild activity against few bacterial strainsμg/ml. The compounds of electron releasing imidazole derivatives (3ii, 3iv, 3viii, 3ix, 3x and xi) presented comparatively better anti-fungal activity than the compounds of electron withdrawing imidazole derivatives (3iii, 3vii and 3xii). Conclusion: The biological activity result revealed that all the newly synthetic compounds 3i-xii [4-(biphenyl-4-yl)-2-(substituted phenyl)-1H-imidazole] exhibited better antibacterial activity as compared to antifungal activity in compare to reference drug.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.