Studies on synthesis, characterization and Biological activity of some nitrogen containing Heterocyclic compounds

Rai, Sankappa U (2012) Studies on synthesis, characterization and Biological activity of some nitrogen containing Heterocyclic compounds. Phd. Thesis thesis, Manipal Institute of Technology, Manipal.

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Nowadays, the alarming rates of emerging and re-emerging microbial threats coupled with increasing antituberculosis, antibacterial and antifungal resistance; particularly in regard to multi drug-resistant microbes are major concerns to the public health as well as scientific communities worldwide. A search for new antimicrobial compounds with a more selective activity and lower toxicity continues to be an area of investigation in medicinal chemistry. It is important to find out newer, safer and more effective antibiotics with broad-spectrum of activity. Heterocyclic compounds by virtue of their specific activity could be employed in the treatment of infectious diseases Review of literature indicated that nitrogen containing heterocycles find a significant place in the development of pharmacologically important molecules. Keeping in view of these observations it was planned to synthesize some nitrogen containing heterocycles. Thus, in this research work, we are presenting the synthesis and preliminary microbiological evaluation of nitrogen containing heterocycles. The present research work involves synthesis, characterization and biological studies of new nitrogen heterocycles carrying interesting pharmacophore like chromeno-pyrimidines, chromeno-oxadiazoles, pyrazolo-oxadiazoles, β- aminoketones and homoallylamines. The study of structure-activity relationship of the new compounds will impart structural elements for new drug designing. Also, the results of research may be useful in understanding the mechanism of drug action.The synthetic methods have been optimized for the new derivatives [chromenopyrimidines (160 a-l) chromeno-oxadiazoles (210 a-n), pyrazolo-oxadiazoles (263 a-k), β- aminoketones (331 a-q) and homoallylamines (335 a-l)]. Structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, mass spectral studies and also by C, H, N elemental analyses. The newly synthesized compounds were tested for their antimicrobial activity. Some of the synthesized compounds were found to exhibit potent activity. Molecular docking studies of few of the synthesized compounds were carried out for better understanding of the drug-receptor interaction. In silico studies were in agreement with the in vitro results.

Item Type: Thesis (Phd. Thesis)
Uncontrolled Keywords: Chromeno-pyrimidines, Chromeno-oxadiazoles, Pyrazolo-oxadiazoles, β- Aminoketones and Homoallylamines, Biological studies, Molecular docking studies.
Subjects: Engineering > MIT Manipal > Chemistry
Depositing User: MIT Library
Date Deposited: 21 Apr 2016 08:53
Last Modified: 21 Apr 2016 08:53

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