Synthesis and Biological Evaluation of Some Diverse Dyhdropyrimidine Dervatives
Keywords:
Dihydropyrimidines, Antitubercular Activity, Antimycobacterial Activity.Abstract
A novel series of dihydropyrimidine derivatives were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. Two compounds, ethyl 4-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate 4a and ethyl 4-[3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate 4d were found to be the most active compounds in vitro with MIC of 0.02 µg/mL against MTB and were 18 times more potent than isoniazid.
References
- Global tuberculosis control - surveillance, planning, financing, WHO Report 2004, please see: http://www.who.int/tb/publications/global_report/en/.
- Revised WHO Fact Sheet No. 104, March 2004; please see: http://www.who.int/mediacentre/factsheets/fs104/en/.
- Global Alliance for TB Drug Development. In Scientific Blueprint for Tuberculosis Drug Development, 2001, please see: http://www.tballiance.org/.
- Parrish, N. M.; Dick, J. D.; Bishai, W. R. Trends Microbiol., 1998, 6, 107.
- Cole, S. T.; Brosch, R.; Parkhill, J. Garnier, T.; Churcher, C.; Harris, D.; Gordon, S. V.; Eiglmeier, K.; Gas, S.; Barry, C.E. 3rd; Tekaia, F.; Badcock, K.; Basham, D.; Brown, D.; Chillingworth, T.; Connor, R.; Davies, R.; Devlin, K.; Feltwell, T.; Gentles, S.; Hamlin, N.; Holroyd, S.; Hornsby, T.; Jagels, K.; Krogh, A.; McLean, J.; Moule, S.; Murphy, L.; Oliver, K.; Osborne, J.; Quail, M. A.; Rajandream, M. A.; Rogers, J.; Rutter, S.; Seeger, K.; Skelton, J.; Squares, R.; Squares, S.; Sulston, J. E.; Taylor, K.; Whitehead, S.; Barrell, B. G. Nature, 1998, 393, 537.
- Clifton, E. B.; Slayden, R. A.; Sampson, A. E.; Lee, R. E. Biochem. Pharmacol., 2000, 59, 221.
- Trivedi, A. R.; Siddiqui, A. B.; Shah, V. H. ARKIVOC, 2008, 2, 210.
- Trivedi, A. R.; Dodiya, D. K.; Ravat, N. R.; Shah, V. H. ARKIVOC, 2008, 11, 131.
- Trivedi, A.; Dodiya, D.; Surani, J.; Mathukia, H.; Ravat, N.; Shah, V. Archiv der pharmazie, 2008, 34, 435.
- Prakash, O.; Pannu, K.; Naithani, R.; Kaur, H. Synthetic Communications, 2006, 36, 3479.
- Collins L.; Franzblau S. G. Antimicrob Agents Chemother, 2007, 41, 1004.
- Orme, I.; Secrist, J.; Anathan, S.; Kwong, C.; maddry, J.; Reynolds, R.; Poffenberger, A.; Michael, M.; Moller, L.; Krahenbuh, J.; Adams, L.; Biswas, A.; Franzblau, S.; Rouse, D.; Winfield, D.; Brooks, J. Antimicrob Agents Chemother, 2001, 45, 1943.
Downloads
Published
Issue
Section
License
Copyright (c) IJSRSET

This work is licensed under a Creative Commons Attribution 4.0 International License.