Isoindolines and Isoindoline-1,3-diones as Nonpeptide ACE Inhibitors: An In Silico and In Vitro Modeling Approach Hypertension, a major cardiovascular risk factor, is often treated with peptide-derived angiotensin-converting enzyme inhibitors (ACEi), which can have several side effects. This study examined a new alternative: isoindoline and isoindoline-1,3-dione derivatives as nonpeptide ACE inhibitors. The synthesis and testing of these compounds involved both in silico molecular docking studies and optimized in vitro inhibitory kinetic assays, along with acute toxicity tests in mice. isoindoline-1,3-dione, D-05, demonstrated the strongest ACE inhibition in vitro (IC50 = 416.4 μM) and effectively bound to the enzyme’s catalytic active site in silico. Additionally, isoindoline-1,3-diones showed lower toxicity in mice (LD50 > 1600 mg/kg) compared to isoindolines (LD50 < 1000 mg/kg). This reduced toxicity is attributed to the presence of fewer reactive secondary metabolites. These promising results highlight the potential of isoindoline-1,3-diones as innovative nonpeptide ACE inhibitors and support further in vivo studies to verify their antihypertensive effects.

Isoindolines and Isoindoline-1,3-diones as Nonpeptide ACE Inhibitors: An In Silico and In Vitro Modeling Approach

pubs.acs.org/doi/10.1021/...

#KellyChibale #MedicinalChemistry #Hypertension #CardiovascularResearch #ACEInhibitors #DrugDiscovery #ComputationalChemistry

RAAS Inhibitors: ACE Inhibitors vs ARBs (1st & 2nd Choice), Uses, Side Effects
#pharmacology #medicine #nursing #kidney #iprkashmishra #raas #aceinhibitors #hypertension #heartfailure #nephrology #nurselife #medstudent

ACE Inhibitors Market Size, Share, Trends Report 2035 ACE Inhibitors Market reach USD 7.76 Billion, at a CAGR of 3.40% by 2035 by growing Demand, Application, industry size, share, sales, revenue, top players trends, technology and forecast 2035 | Angiot...

❤️ Hypertension management drives the #ACEInhibitors market forward! 🔗 www.marketresearchfuture.com/reports/ace-...

#pharmacology11
#RAASInhibitors #ACEInhibitors #ARBs #Pharmacology #NursingStudents #MedicalEducation #Hypertension #HeartFailure #MyocardialInfarction #NCLEXPrep #MedSchoolLife #PharmaFacts #NursingNotes #StudyMedicine #HealthcareEducation

ACE Inhibitors Market Size, Share, Trends Report 2034 ACE Inhibitors Market reach USD 7.76 Billion, at a CAGR of 3.40% by 2034 by growing Demand, Application, industry size, share, sales, revenue, top players trends, technology and forecast 2034 | Angiot...

❤️‍🩹 Protecting hearts worldwide! The #ACEInhibitors market remains vital in managing #Hypertension & cardiovascular health 💊🌍
#CardioCare #PharmaTrends #HeartHealth

www.marketresearchfuture.com/reports/ace-...

Our researchers have discovered the commonly-used antibiotic ciprofloxacin could be used as a template for a new family of blood pressure drugs. #ACEinhibitors www.bath.ac.uk/announcement...

What is the Link Between Diabetes and Kidney Disease?


#ACEinhibitors #ARBs #artificialintelligence #biomarkers #BloodSugarControl #chronickidneydisease #CKD #diabetes #diabeticnephropathy #dialysis #GeneticStudies #GFR #glomerularfiltrationrate #Hypertension
thediabeticwriter.com/?p=6293