Display options
Cite
Kumarachari RK, Peta S, Surur AS, et al. Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines. J Pharm Bioallied Sci. 2016;8(3):181-7doi: 10.4103/0975-7406.171678.
Kumarachari, R. K., Peta, S., Surur, A. S., & Mekonnen, Y. T. (2016). Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines. Journal of pharmacy & bioallied sciences, 8(3), 181-7. https://doi.org/10.4103/0975-7406.171678
Kumarachari, Rajasekhar Komarla, et al. "Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines." Journal of pharmacy & bioallied sciences vol. 8,3 (2016): 181-7. doi: https://doi.org/10.4103/0975-7406.171678
Kumarachari RK, Peta S, Surur AS, Mekonnen YT. Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines. J Pharm Bioallied Sci. 2016 Jul-Sep;8(3):181-7. doi: 10.4103/0975-7406.171678. PMID: 27413345; PMCID: PMC4929956.
Copy Download .nbib Format: NLM
Share it on

J Pharm Bioallied Sci. 2016 Jul-Sep;8(3):181-7. doi: 10.4103/0975-7406.171678.

Synthesis, characterization and in silico biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines.

Journal of pharmacy & bioallied sciences

Rajasekhar Komarla Kumarachari, Sivakumar Peta, Abdrrahman Shemsu Surur, Yenus Tadesse Mekonnen

Affiliations

  1. Department of Pharmaceutical Chemistry, School of Pharmacy, College of Medicine and Health Sciences, University of Gondar, India.
  2. Department of Pharmaceutical Chemistry, Gokula Krishna College of Pharmacy, Sullurpeta, Andhra Pradesh, India.

PMID: 27413345 PMCID: PMC4929956 DOI: 10.4103/0975-7406.171678

Abstract

INTRODUCTION: As pyrimidine is a basic nucleus in DNA and RNA, it has been found to be associated with diverse biological activities. Pyrimidine derivatives were reported to possess anticonvulsant, antimicrobial, anti-inflammatory, antitumor, and antihistaminic. Recently, our team reported the anti-inflammatory and antimicrobial evaluation of some pyrimidines.

OBJECTIVE: To synthesize, predict and evaluate biological activity of some 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines.

EXPERIMENTAL: seven new pyrimidines were synthesized by following the standard procedures using substituted aromatic aldehydes, methyl ketones and metformin. After the biological activity was predicted using PASS, Molinspiration and Osiris property explorer, their anthelmintic activity was evaluated using Pheretima posthuma. The structural assignment of the title compounds (P1-7) has been made on the basis of elemental analysis, infrared, 1H-nuclear magnetic resonance and Mass spectral studies.

RESULTS: All the synthesized compounds were found to obey Lipinski's rule. All the synthesized compounds scored good bioactivity values as GPCR ligands and kinase inhibitors. Among the test compounds, P5 was found to be more potent anthelmintic inducing paralysis in 36-48 minutes and death in 40-51 minutes.

CONCLUSION AND RECOMMENDATION: The synthesized compound (P5) possessing methoxy group at position-4 of the benzene ring located at position-4 of pyrimidine exhibited good anthelmintic activity. The study revealed the necessity of synthesizing many more compounds with other substituents at position-4 of the benzene ring located at position-4 of pyrimidine.

Keywords: 2-(N,N-dimethyl guanidinyl)-4,6-diaryl pyrimidines; Molinspiration; Osiris; PASS; anthelmintic activity

References

  1. J Med Chem. 2000 Oct 5;43(20):3714-7 - PubMed
  2. Arch Pharm Res. 2007 Dec;30(12):1511-20 - PubMed
  3. Eur J Med Chem. 2009 Dec;44(12):4787-92 - PubMed
  4. Saudi Pharm J. 2009 Jul;17(3):255-8 - PubMed

Publication Types