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

Authors :
Pankaj K. Bagul
Ravindra M. Kumbhare
Umesh B. Kosurkar
Abhinav Kanwal
Tulshiram L. Dadmal
Sanjay K. Banerjee
K. Appalanaidu
Source :
Bioorganicmedicinal chemistry. 22(21)
Publication Year :
2014

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 6 h, 6 i and 6 j 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.

Details

ISSN :
14643391
Volume :
22
Issue :
21
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry
Accession number :
edsair.doi.dedup.....dcd591e576d21ff2cf284972160df383