Synthesis of Several Dihydropyrimidines as Antimycobacterial Agents

Authors(1) :-Nirul V. Gothi

A small series of 30 dihydropyrimidine compounds were synthesized and assessed for their in vitro antimycobacterial potential against Mycobacterium tuberculosis H37Rv. The lowest MIC value, 0.02 g/mL, was found for compounds 4a and 4d. Both the compounds showed comparatively low cytotoxicity, and were potent against M. tuberculosis strains resilient to known drugs.

Authors and Affiliations

Nirul V. Gothi
Arts, Science & R. A. Patel commerce college, Bhadran, Gujarat, India

Dihydropyrimidines; Antimycobacterial activity; MDR-TB.

  1. Corbett EL, Watt CJ, Walker N (2003) The growing burden of tuberculosis: global trends and interactions with the HIV epidemic. Arch Intern Med 163:1009-1021.
  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 (2003) American Thoracic Society/Centers for Disease Control and Prevention/ Infectious Diseases Society of America: treatment of tuberculosis. Am J Respir Crit CareMed 167:603–662.
  3. Yew WW (1999) Directly Observed Therapy, Short-Course: The Best Way to Prevent Multidrug- Resistant Tuberculosis. Chemotherapy 45:26-33.
  4. Trivedi AR, Siddiqui AB, Shah VH (2008) Design synthesis characterization and antitubercular activity of some newer 2-hetrocycle phenothiazines. ARKIVOC 2:210-217.
  5. Trivedi AR, Dodiya DK, Ravat NR, Shah VH (2008) Synthesis and biological evaluation of some new pyrimidines via a novel chalcone series. ARKIVOC 11:131-.
  6. Trivedi A, Dodiya D, Surani J, Mathukia H, Ravat N, Shah V (2008) Facile one-pot synthesis and antimycobacterial evaluation of pyrazolo[3,4-d]pyrimidines. Archiv der pharmazie 341:435-439.
  7. Collins L, Franzblau SG (2007) Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob Agents Chemother 41:1004-1009.
  8. (a) Basso LA, Blanchard JS (1998) Resistance to Antitubercular Drugs. Adv Exp Med Biol 456:115-144. (b) Bradford WZ, Daley CL (1998) Multiple Drug-Resistant Tuberculosis. Infect Dis Clin North Am 12:157-172. (c) Bastian I, Colebunders R (1999) Treatment and Prevention of Multidrug-Resistant Tuberculosis. Drugs 58:633-666. (d) Cohn DL, Bustreo F, Raviglione, MC (1997) Drug-Resistant Tuberculosis: Review of the Worldwide Situation and the WHO/IUATLD Global Surveillance Project. Clin Infect Dis 24:121-130.
  9. Sung, SW, Kang CH. Kim YT, Han SK, Shim YS, Kim JH (1999) Surgery increased the chance of cure in multi-drug resistant pulmonary tuberculosis. Eur J Cardiothorac Surg 16:187-193.

Publication Details

Published in : Volume 1 | Issue 1 | January-Febuary 2015
Date of Publication : 2015-02-27
License:  This work is licensed under a Creative Commons Attribution 4.0 International License.
Page(s) : 410-414
Manuscript Number : IJSRSET184106
Publisher : Technoscience Academy

Print ISSN : 2395-1990, Online ISSN : 2394-4099

Cite This Article :

Nirul V. Gothi, " Synthesis of Several Dihydropyrimidines as Antimycobacterial Agents, International Journal of Scientific Research in Science, Engineering and Technology(IJSRSET), Print ISSN : 2395-1990, Online ISSN : 2394-4099, Volume 1, Issue 1, pp.410-414, January-Febuary-2015.
Journal URL : http://ijsrset.com/IJSRSET184106

Article Preview

Follow Us

Contact Us