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Elsevier, Bioorganic and Medicinal Chemistry, 21(22), p. 5824-5830, 2014

DOI: 10.1016/j.bmc.2014.09.027

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

Journal article published in 2014 by Ravindra M. Kumbhare, Umesh B. Kosurkar, Pankaj K. Bagul, Abhinav Kanwal, K. Appalanaidu, Tulshiram L. Dadmal, Sanjay Kumar Banerjee ORCID
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This paper is available in a repository.

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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 0.713μM, 0.409μM and 0.653μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928μM.