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Synthesis, characterization of biologically potent novel chalcones bearing urea, thiourea and acetamide linkages

Mewada N. S., Shah D. R., Chikhalia K. H.

International Letters of Chemistry, Physics and Astronomy

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2014

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Vol. 17, iss. 3

281--294

EN

Three series of some novel chalcone based urea, thiourea and acetamide derivatives were designed, synthesized and screened for their antimicrobial and antifungal activities. All the synthesized compounds are first reported. The structures of the compounds were elucidated with the aid of elemental analysis and spectral methods including IR, 1H-NMR spectral data. The prepared compounds were evaluated for antibacterial activity against two Gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus), two Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also investigated for their antifungal activity using the broth micro dilution method. The bioassay results showed that compounds a few compounds showed good to superior in vitro antibacterial and antifungal activity.

2

Synthesis and in vitro antimicrobial evaluation of amine substituted s-triazine based thiazolidinone/chalcone hybrids

Shah D. R., Lakum H. P., Chikhalia K. H.

International Letters of Chemistry, Physics and Astronomy

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2014

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Vol. 17, iss. 2

207--219

EN

In an attempt to control multidrug resistant dilemma, a library of s-triazine based on two novel series of thiazolidinone (4a-e) and chalcone (7a-e) derivatives were designed and synthesized with simple and efficient etiquette. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus Aureus, Bacillus Cereus, Pseudomonas Aeruginosa, Klebsiella Pneumoniae,) and fungi (Candida Albicans, Aspergillus Clavatus) using the broth dilution technique. Compound 7d was the best bioactive desired antibacterial analogue with less MIC value against different tested strains. Results of bioassay study revealed the future hope of the potent drug-candidate based on s-triazine scaffold. All the final synthesized compounds were characterized by IR, 1 H NMR, 13 C NMR, mass and elemental analysis.

3

Novel s-Triazinyl Schiff Base/Chalcone Congeners: Rational, Synthesis, Antimicrobial and Anti-TB Evaluation

Lakum H. P., Shah D. R., Chikhalia K. H.

International Letters of Chemistry, Physics and Astronomy

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2014

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Vol. 19, iss. 1

56--73

EN

The occurrence of Multi Drug Resistant (MDR) infectious microbial strains has been increased upto alarming level which affects the public health worldwide. To cure this problem, a library of s-triazinyl derivatives comprising schiff base or chalcone motif have been rationalized, synthesized and screened for their in vitro antibacterial activity against five bacterial strains (Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 441, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 741 and Klebsiella pneumoniae MTCC 109) and four fungal strains (Aspergillus niger MTCC 282, Aspergillus fumigates MTCC 343, Aspergillus clavatus MTCC 1323, Candida albicans MTCC 183) using broth dilution technique. All the newly synthesized scaffolds were further evaluated for their in vitro anti-TB efficacy against the tubercular strain (Mycobacterium tuberculosis H37Rv) using Lowenstein-Jensen MIC method. All the derivatives were well characterized by IR, 1H NMR, 13C NMR, elemental analysis as well as mass spectroscopy.