Synthesis, Characterization and Biological Screening of Some Novel Triazolopyrimidine Derivatives Possessing Isopropyl Group

Authors

  • Janaki H. Chauhan  Tolani College of Arts and Science, Gandhidham, Gujarat, India
  • Dr. Haresh K. Ram  Tolani College of Arts and Science, Gandhidham, Gujarat, India

DOI:

https://doi.org/10.32628/IJSRST207276

Keywords:

3-amino-1,2,4-triazole, N N-(3-chloro-4-fluorophenyl)-4-methyl-3-oxopentanamide and DMF.

Abstract

Well organized Synthesis of a completely new series of N-(3-chloro-4-fluorophenyl)-7-(substitutedchlorophenyl)-4,7-dihydro-5-isopropyl-[1,2,4]triazolo [1,5-a]pyrimidine-6-carboxamide (4a-j) was achieved from condensation reaction of N-(3-chloro-4-fluorophenyl)-4-methyl-3-oxopentanamide, 3-amino-1,2,4-triazole and different aldehyde. After refluxing of 20 minutes with DMF and cooling product is obtained. these new compounds were characterized using some physical techniques like FT-IR spectra, Mass spectra, by the 1H-NMR spectra. Antimicrobial activity and antifungal activity were studied against example of gram -positive gram- negative bacterial and fungal strain.

References

  1. Ulaczyk-Lesanko, A.; Hall, D. G. Wanted. New multicomponent reactions for generating libraries of polycyclic natural products. Curr. Opin. Chem. Biol., 2005, 9, 266-276.
  2. Tietze, L. F.; Lieb, M. E. Domino reactions for library synthesis of small molecules in combinatorial chemistry. Curr. Opin. Chem. Biol., 1998, 2, 363-371.
  3. Biginelli, P. Aldureides of ethylic acetoacetate and ethylic oxalacetate. Gazz. Chim. Ital., 1893, 23, 360-416.
  4. Mayer, T. M.; Kapoor, T. M.; Haggarty, S. J.; King, R. W.; Schreiber, S. L.; Mitchison, T. J. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science, 1999, 286, 971-974.
  5. Garcia-Saez, I.; DeBonis, S.; Lopez, R.; Trucco, F.; Rousseau, B.; Thuéry, P.; Kozielski, F. Structure of human Eg5 in complex with a new monastrolbased inhibitor bound in the R configuration. J. Biol. Chem., 2007, 282, 9740-9747.
  6. Atwal, K. S.; Swanson, B. N.; Unger, S. E.; Floyd, D. M.; Moreland, S.; Hedberg, A.; O’Reilly, B. C. Dihydropyrimidine calcium channel blockers. 3-Carbamoyl-4-aryl-1,2,3,4-tetrahydro-6-methyl-5-pyrimidinecarboxylic acid esters as orally effective antihypertensive agents. J. Med. Chem., 1991, 34, 806-811.
  7. Kappe, C. O. Biologically active dihydropyrimidones of the Biginelli-type - a literature survey. Eur. J. Med. Chem., 2000, 35, 1043-1052.
  8.  Singh, K.; Arora, D.; Singh, K.; Singh, S. Genesis of dihydropyrimidinone calcium channel blockers: recent progress in structure-activity relationships and other effects. Mini Rev. Med. Chem., 2009, 1, 95-106.
  9. Kim, S. S.; Choi, B. S.; Lee, J. H.; Lee, K. K.; Lee, T. H.; Kim, Y. H.; Hyunik, S. Oxidation of Biginelli reaction products: Synthesis of 2- unsubstituted 1,4-dihydropyrimidines, pyrimidines, and 2- hydroxypyrimidines. Synlett, 2009, 599-602.
  10. Yamamoto, K.; Chen, Y. G.; Buono, F. G. Oxidative dehydrogenation of dihydropyrimidinones and dihydropyrimidines. Org. Lett., 2005, 7, 4673- 4676.
  11. Wang, X.-C.; Quan, Z.-J.; Zhang, Z. Michael additions of dihydropyrimidines and 2-amino-1,3,4-thiadiazoles to _ ,_-ethylenic compounds: using polyethylene glycols as a green reaction media. Tetrahedron, 2007, 63, 8227-8233.
  12. National Committee for Clinical and Laboratory Standards, Method for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically Approved Standard, fourth ed. NCCLS, Villanova, Italy, Document M 100-S7, S100-S157 (1997).
  13. D.H. Isenberg, Essential Procedure for Clinical Microbiology, American Society for Microbiology, Washington, (1998).
  14. J. R.Zgoda, J. R. Porter, Pharm. Biol., 39, 221-225 (2001).

International Journal of Scientific Research in Science and Technology

Downloads

Published

2019-05-20

Issue

Volume 6, Issue 3, May-June-2019

Section

Research Articles

License

Copyright (c) IJSRST

Creative Commons License

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

How to Cite

[1]
Janaki H. Chauhan, Dr. Haresh K. Ram "Synthesis, Characterization and Biological Screening of Some Novel Triazolopyrimidine Derivatives Possessing Isopropyl Group" International Journal of Scientific Research in Science and Technology(IJSRST), Online ISSN : 2395-602X, Print ISSN : 2395-6011,Volume 6, Issue 3, pp.386-391, May-June-2019. Available at doi : https://doi.org/10.32628/IJSRST207276