A Versatile Approach for Synthesis of Various Pyrimidine Derivatives Clubbed with Pyrazolone Structure and Their Biological Activities

Authors

  • Amish P. Khamar  Arts, Science & R. A. Patel Commerce College, Bhadran, Gujarat, India

Keywords:

Pyrazolopyrimidines, Antitubercular Activity, Antimycobacterial Activity, MABA Assay.

Abstract

Different pyrimidine derivatives clubbed with pyrazolone structure possessing a diversity of substituents in the 6-position have been synthesized and evaluated for Mycobacterium tuberculosis activities. Several compounds demonstrated IC90 ≤ 10 µg/mL and were found to be active against Mycobacterium tuberculosis strain Compound 8d was found to be most active compound in vitro with IC90 of 1.53.

References

  1. Corbett EL, Watt CJ, Walker N. The growing burden of tuberculosis: global trends and interactions with the HIV epidemic. Arch Intern Med 2003;163:1009-21.
  2. Blumberg HM, Burman WJ, Chaisson RE, Daley CL, Etkind SC, Friedman LN, Fujiwara P, Grzemska M, Hopewell PC, Iseman MD, Jasmer RM, Koppaka V, Menzies RI, O’Brien RJ, Reves RR, Reichman LB, Simone PM, Starke JR, Vernon AA. American Thoracic Society/Centers for Disease Control and Prevention/ Infectious Diseases Society of America: treatment of tuberculosis. Am J Respir Crit CareMed 2003;167:603-62.
  3. Yew WW. Directly Observed Therapy, Short-Course: The Best Way to Prevent Multidrug- Resistant Tuberculosis. Chemotherapy 1999;45:26-33.
  4. Trivedi AR, Siddiqui AB, Shah VH. Design synthesis characterization and antitubercular activity of some newer 2-hetrocycle phenothiazines. ARKIVOC 2008;2:210-17.
  5. Trivedi AR, Dodiya DK, Ravat NR, Shah VH. Synthesis and biological evaluation of some new pyrimidines via a novel chalcone series. ARKIVOC 2008;11:131-37.
  6. Trivedi A, Dodiya D, Surani J, Mathukia H, Ravat N, Shah V. Facile one-pot synthesis and antimycobacterial evaluation of pyrazolo[3,4-d]pyrimidines. Archiv der pharmazie 2008;341:435-39.
  7. Collins L, Franzblau SG. Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob Agents Chemother 2007;41:1004-1009.
  8. Tiwari S, Khupse N, Kumar A. Intramolecular Diels-Alder reaction in ionic liquids: effect of ion-specific solvent friction. Journal of organic chemistry 2008;73:9075-83.

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Published

2017-02-28

Issue

Section

Research Articles

How to Cite

[1]
Amish P. Khamar, " A Versatile Approach for Synthesis of Various Pyrimidine Derivatives Clubbed with Pyrazolone Structure and Their Biological Activities, International Journal of Scientific Research in Science and Technology(IJSRST), Online ISSN : 2395-602X, Print ISSN : 2395-6011, Volume 3, Issue 1, pp.658-665, January-February-2017.