Back to Search
Start Over
Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors
- 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.
- Subjects :
- Dihydropyridines
Stereochemistry
Cell Survival
Clinical Biochemistry
Triazole
Pharmaceutical Science
Angiotensin-Converting Enzyme Inhibitors
Peptidyl-Dipeptidase A
Biochemistry
Mannich Bases
chemistry.chemical_compound
Cell Line, Tumor
Drug Discovery
medicine
Ic50 values
Humans
Molecular Biology
IC50
Ace inhibition
biology
Chemistry
Organic Chemistry
Dihydropyridine
Angiotensin-converting enzyme
Triazoles
Enzyme Activation
HEK293 Cells
Ace inhibitory
ACE inhibitor
biology.protein
Molecular Medicine
medicine.drug
Protein Binding
Subjects
Details
- ISSN :
- 14643391
- Volume :
- 22
- Issue :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry
- Accession number :
- edsair.doi.dedup.....dcd591e576d21ff2cf284972160df383