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

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

  • Bioorg Med Chem. 2014 Nov 1;22(21):5824-30. doi: 10.1016/j.bmc.2014.09.027.
Ravindra M Kumbhare 1,  Umesh B Kosurkar 2,  Pankaj K Bagul 3,  Abhinav Kanwal 3,  K Appalanaidu 2,  Tulshiram L Dadmal 2,  Sanjay Kumar Banerjee 4
Affiliations

Affiliations

  • 1 Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India. Electronic address: kumbhare@iict.res.in.
  • 2 Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India.
  • 3 Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India; Present Address: Drug Discovery Research Center (DDRC), Translational Health Science and Technology Institute (THSTI), Gurgaon 122016, India.
  • 4 Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India; Present Address: Drug Discovery Research Center (DDRC), Translational Health Science and Technology Institute (THSTI), Gurgaon 122016, India. Electronic address: skbanerjee@thsti.res.in.
PMID: 25300819 DOI: 10.1016/j.bmc.2014.09.027
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.

Keywords

1,4-Dihydropyridine; Angiotensin converting enzyme; Inhibitors; Mannich bases; Triazole.

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