Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.

doi:10.1016/j.bmc.2015.04.024

Paper

Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.

Published Jul 1, 2015 · A. Jallapally, Dinesh Addla, Pankaj K. Bagul

Bioorganic & medicinal chemistry

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7

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Abstract

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In Vitro Study

Study Snapshot

Novel 2-butyl-4-chloroimidazole peptidomimetics show potent Angiotensin Converting Enzyme (ACE) inhibitor activity, with 5i being the most active with greater potency than marketed drugs Lisinopril and Ramipril.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.

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References

Burden of Cardiovascular Morbidity and Mortality Following Humanitarian Emergencies: A Systematic Literature Review

Humanitarian emergencies can lead to increased cardiac morbidity and mortality, persisting for years after the event.

New Perspectives in the Renin-Angiotensin-Aldosterone System (RAAS) I: Endogenous Angiotensin Converting Enzyme (ACE) Inhibition

An endogenous ACE inhibitor, similar to ACE inhibitory drugs, is present in human serum and is present in various animal species, suggesting its evolutionary conserved nature.

Hypertension and Diabetes: Entry Points for Prevention and Control of the Global Cardiovascular Epidemic

Core interventions, such as multidrug regimens and behavioral modification, are highly cost-effective and feasible for preventing and controlling hypertension and diabetes in resource-constrained settings.

Inhibition of Angiotensin-Converting Enzyme Activity by Flavonoids: Structure-Activity Relationship Studies

Flavonoids, particularly luteolin, show potential as functional antihypertensive products due to their inhibitory effect on angiotensin-converting enzyme activity.

Structure based drug design of angiotensin-I converting enzyme inhibitors.

Structure-based drug design has led to the development of domain-selective ACE inhibitors, which may lead to new therapeutic approaches for treating hypertension and cardiovascular diseases.

Citations

New strategy to design fluorescent substrates of carboxypeptidases using a combination of dansylated peptides and albumin

Dansylated peptides and albumin can effectively design fluorescent substrates for measuring carboxypeptidase activity and inhibitor effectiveness in high-throughput screening.

Current Advances in the Synthesis and Biological Evaluation of Pharmacologically Relevant 1,2,4,5-Tetrasubstituted-1H-Imidazole Derivatives

Recent advances in the synthesis and biological evaluation of 1,2,4,5-tetrasubstituted-1H-imidazole derivatives show potential as drugs for treating various diseases.

Phytochemical profile and angiotensin I converting enzyme (ACE) inhibitory activity of Limonium michelsonii Lincz

Limonium michelsonii Lincz contains flavonol glycosides 16-20, which show potent angiotensin I converting enzyme inhibitory activity, potentially improving blood circulation and promoting health benefits.

Structural characterization of two tetrachloridozincate salts of 4-carboxy-1H-imidazol-3-ium: a salt hydrate and a co-crystal salt hydrate

The first crystallizes with a single water molecule, while the second crystallizes with two equivalents of zwitterion 4-carboxy-1H-imidazole per salt formula unit.

Ionic Liquid Solvation versus Catalysis: Computational Insight from a Multisubstituted Imidazole Synthesis in [Et2NH2][HSO4]

Ionic liquids can act as both solvents and catalysts in imidazole synthesis, reducing energy barriers and promoting reaction progress.