Synthesis and evaluation of chalcone analogues based pyrimidines as angiotensin converting enzyme inhibitors

Bukhari Syed Nasir Abbas, A. M. Butt, M. W B Amjad, W. Ahmad, V. H. Shah, A. R. Trivedi

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Hypertension is a widespread and frequently progressive ailment that imparts a foremost threat for cardiovascular and renal disorders. Mammoth efforts are needed for the synthesis of innovative antihypertensive agents to combat this lethal disease. Chalcones have shown antihypertensive activity through inhibition of Angiotensin Converting Enzyme (ACE). Hence, a series of chalcone analogues is synthesized and used as precursor for the synthesis of novel series of pyrimidines. Precursor chalcones were prepared by reacting aldehydes and ketones in presence of sodium hydroxide followed by synthesis of corresponding pyrimidines by reaction with urea in presence of potassium hydroxide. Both groups were then evaluated for their effects on ACE. The results depicted that pyrimidines were more active than chalcones with methoxy (C5 and P5) substitution showing best results to inhibit ACE. Given that chalcone analogues and pyrimidines show a potential as the angiotensin converting enzyme inhibitors.

Original languageEnglish
Pages (from-to)1368-1372
Number of pages5
JournalPakistan Journal of Biological Sciences
Volume16
Issue number21
DOIs
Publication statusPublished - 2013

Fingerprint

chalcone
pyrimidines
chalcones
peptidyl-dipeptidase A
synthesis
potassium hydroxide
antihypertensive effect
antihypertensive agents
sodium hydroxide
ketones
aldehydes
hypertension
urea
kidneys
angiotensin-converting enzyme inhibitors

Keywords

  • ACE inhibitors
  • Chalcones
  • Hypertension
  • Pyrimidines
  • Renin-angiotensin system

ASJC Scopus subject areas

  • Agronomy and Crop Science

Cite this

Synthesis and evaluation of chalcone analogues based pyrimidines as angiotensin converting enzyme inhibitors. / Syed Nasir Abbas, Bukhari; Butt, A. M.; Amjad, M. W B; Ahmad, W.; Shah, V. H.; Trivedi, A. R.

In: Pakistan Journal of Biological Sciences, Vol. 16, No. 21, 2013, p. 1368-1372.

Research output: Contribution to journalArticle

Syed Nasir Abbas, Bukhari ; Butt, A. M. ; Amjad, M. W B ; Ahmad, W. ; Shah, V. H. ; Trivedi, A. R. / Synthesis and evaluation of chalcone analogues based pyrimidines as angiotensin converting enzyme inhibitors. In: Pakistan Journal of Biological Sciences. 2013 ; Vol. 16, No. 21. pp. 1368-1372.
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AU - Shah, V. H.

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