20224-08-2Relevant articles and documents
Synthesis, antimicrobial and cytotoxic activity of 2-azetidinone derivatives of pyridyl benzimidazoles
Desai,Pandya,Kotadiya,Desai, Priyanka
, p. 1725 - 1741 (2014)
In the present study, a series of novel 6-(1H-benzo[d]imidazol-2-yl)-2-(3- chloro-2-oxo-4-phenylazetidin-1-yl)-4-(aryl)nicotinonitriles 6a-o were efficiently synthesized and evaluated for their in vitro antibacterial activity against Gram-positive (Staphylococcus aureus and Streptococcus pyogenes), Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria and fungal (Candida albicans, Aspergillus niger and Aspergillus clavatus) strains. The results of antimicrobial study revealed that compounds 6b, 6c, 6d, 6h and 6i exhibited substantial antibacterial activity while compounds 6c and 6h emerged as the most potent antifungal agents compared to the standard drugs chloramphenicol and ketoconazole, respectively. From the standpoint of SAR studies, it was observed that the presence of electron-withdrawing groups remarkably enhances the antibacterial activity of newly synthesized compounds. Further, the results of preliminary MTT cytotoxicity studies on HeLa cells suggested that potent antimicrobial activity of 6b, 6c, 6d, 6h and 6i is accompanied by low level of cytotoxic concentrations. All the newly synthesized analogues were characterized by IR, 1H NMR, 13C NMR and mass spectral data. Springer Science+Business Media 2013.
Synthesis and characterization of novel benzimidazole bearing pyrazoline derivatives as potential antimicrobial agents
Desai,Pandya,Kotadiya,Desai, Priyanka
, p. 1474 - 1487 (2014/03/21)
A new series of compounds N-(4-(2-(3-(1H-benzo[d]imidazol-2-yl)-5-(aryl)-4, 5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy)phenyl)acetamides (5a-u) were synthesized and structures of these compounds were elucidated by spectral (IR, 1H NMR, 13C NMR, and mass spectra) analysis. Antimicrobial activity was measured against Escherichia coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442), Candida albicans (MTCC 227), Aspergillus niger (MTCC 282), and Aspergillus clavatus (MTCC 1323) by serial broth dilution method. Evaluation of antimicrobial activity revealed that compounds 5f, 5i, 5q, and 5t were the most active antibacterial, while compounds 5e, 5g, 5h, 5j, 5p, 5r, and 5u were the most potent antifungal agents as compared to standard drugs and thus could be promising new lead molecules.
Synthesis, antimicrobial, and cytotoxic activities of novel benzimidazole derivatives bearing cyanopyridine and 4-thiazolidinone motifs
Desai,Pandya,Bhatt,Kotadiya,Desai, Priyanka
, p. 3823 - 3835 (2014/08/05)
A series of 6-(1H-benzo[d]imidazol-2-yl)-2-(2-(3-nitrophenyl)-4- oxothiazolidin-yl)-4-(aryl)nicotinonitriles 5a-l were synthesized and characterized by IR, 1H NMR, 13C NMR, and mass spectrometry techniques. These novel compounds 5a-l were screened for their in vitro antimicrobial activity against different bacterial and fungal strains and in vitro cytotoxicity study (HeLa cell line) using MTT colorimetric assay. The results demonstrated that compounds 5c , 5e, and 5i-k exhibited excellent antibacterial activity, while compounds 5d, 5i, and 5k were found to be the most potent antifungal agents. From the standpoint of SAR studies, it was observed that the presence of electron donating groups remarkably enhanced the antimicrobial activity of newly synthesized compounds. Further, the results of preliminary MTT cytotoxicity studies on HeLa cells suggested that potent antimicrobial activity of 5c-e and 5i-k was accompanied by low cytotoxicity. Springer Science+Business Media 2014.
