Skip to main content
padlock icon - secure page this page is secure

Synthesis of Nitrogen and Oxygen based Pyrazole Derivatives and Its Antitubercular and Antimicrobial Activity

Buy Article:

$68.00 + tax (Refund Policy)

Background: Pyrazole, oxazole and pyrimidine are nitrogen containing heterocycles which possess very good binding efficiency with receptor or proteins. Due to this effect it can be work as antitubercular agents with active substituents. The objective of this paper is clubbed the heterocycles to enhance their antitubercular potency. Methods: The active substituted pyrazole aldehydes were synthesized by reaction of phenyl hydrazine with different acetophenone followed by Vilsmeier-Haack formylation reaction. The isoxazole and aminopyrimidines were prepared by condensation of various chalcones with hydroxyl amine hydrochloride and guanidine hydrochloride respectively. The structures of the newly synthesized compounds were characterized by 1H-NMR, Mass, IR and elemental analysis data. All the newly synthesized compounds were screened for their antibacterial activity against Gram-positive S.pyogenus and Gram negative E.coli, Paeruginosa, S.aureus and antitubercular activity against mycobacterium tuberculosis H37Rv. Results: Oxygen containing substituent in aromatic ring or heterocycles as a substituent were enhancing the antitubercular activity as compared to the other substituents. Ethoxy group present as a substituent in aromatic ring shows minimum inhibition concentration as compared to others. Conclusion: X-ray crystallographic study enhances that E-isomer formed in case of chalcones. The electron withdrawing group such as fluorine and chlorine enhancing the activity of Isoxazole and Pyridine as compare to the chalcones. Electron donating group such as ethoxy is increase the potency of the compounds at para position.
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: Aminopyrimidines; Antimicrobial screening; Antitubercular screening; Chalcones; Isoxazoles

Document Type: Research Article

Publication date: August 1, 2015

More about this publication?
  • Anti-Infective Agents publishes original research, expert reviews, drug clinical trial studies and guest edited issues on all the latest and outstanding developments on the medicinal chemistry, biology, pharmacology and use of anti-infective and anti-parasitic agents. The scope of the journal covers all pre-clinical and clinical research on antimicrobials, antibacterials, antiviral, antifungal, and antiparasitic agents. Anti-Infective Agents is an essential journal for all infectious disease researchers in industry, academia and the health services.
  • Editorial Board
  • Information for Authors
  • Submit a Paper
  • Subscribe to this Title
  • Information for Advertisers
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more