SYNTHESIS AND BIOLOGICAL INVESTIGATIONS OF OXA/AZA HETEROCYCLICS
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The development of heterocycles as scaffolds containing a high degree of diversity has become a leading focus in modern drug discovery. In this research program the derivatives of various diverse classes of heterocycles e.g.oxadiazole, triazole and pyrazole were developed. The modification and optimization of reaction conditions, characterization of the structure of newly synthesized compounds and a study of their biological activity would definitely contribute to update the existing knowledge in the field of heterocyclic chemistry. The part of the present work gives an overview of methods of ...
The development of heterocycles as scaffolds containing a high degree of diversity has become a leading focus in modern drug discovery. In this research program the derivatives of various diverse classes of heterocycles e.g.oxadiazole, triazole and pyrazole were developed. The modification and optimization of reaction conditions, characterization of the structure of newly synthesized compounds and a study of their biological activity would definitely contribute to update the existing knowledge in the field of heterocyclic chemistry. The part of the present work gives an overview of methods of the synthesis of substituted triazoles, oxadiazoles and pyrazoles. It will explain how different conditions and structure of substrates can influence the direction for reactions.A brief review of literature has been presented along with the objectives of the work. The anti-bacterial studies revealed that majority of the tested compounds exhibited moderate to good antibacterial activity. The docking study revealed the binding orientation of compounds in the DNA GyrB and Asp kinase of antituberculosis binding pocket surrounding the active site, which resulted in inhibition of enzyme activity.
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