Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors

Ravindra M. Kumbhare, Umesh B. Kosurkar, Pankaj K. Bagul, Abhinav Kanwal, K. Appalanaidu, Tulshiram L. Dadmal, Sanjay Kumar Banerjee

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6h, 6i and 6j to have good ACE inhibition activity with IC50 values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 μM.

Original languageEnglish
Pages (from-to)5824-5830
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number21
DOIs
Publication statusPublished - 01-11-2014

Fingerprint

Mannich Bases
Triazoles
Peptidyl-Dipeptidase A
Angiotensin-Converting Enzyme Inhibitors
Enzyme inhibition
Enzyme activity
Inhibitory Concentration 50
Screening
1,4-dihydropyridine

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Kumbhare, Ravindra M. ; Kosurkar, Umesh B. ; Bagul, Pankaj K. ; Kanwal, Abhinav ; Appalanaidu, K. ; Dadmal, Tulshiram L. ; Banerjee, Sanjay Kumar. / Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors. In: Bioorganic and Medicinal Chemistry. 2014 ; Vol. 22, No. 21. pp. 5824-5830.
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Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors. / Kumbhare, Ravindra M.; Kosurkar, Umesh B.; Bagul, Pankaj K.; Kanwal, Abhinav; Appalanaidu, K.; Dadmal, Tulshiram L.; Banerjee, Sanjay Kumar.

In: Bioorganic and Medicinal Chemistry, Vol. 22, No. 21, 01.11.2014, p. 5824-5830.

Research output: Contribution to journalArticle

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AU - Kumbhare, Ravindra M.

AU - Kosurkar, Umesh B.

AU - Bagul, Pankaj K.

AU - Kanwal, Abhinav

AU - Appalanaidu, K.

AU - Dadmal, Tulshiram L.

AU - Banerjee, Sanjay Kumar

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