Synthesis, crystal structure, molecular docking studies and biological evaluation of aryl substituted dihydroisoquinoline imines as a potent angiotensin converting enzyme inhibitor

Selmi, Awatef; Aydi, Rihab; Kammoun, Omar; Bougatef, Hajer; Bougatef, Ali; Miled, Nabil; Alghamdi, Othman A.; Kammoun, Majed

doi:10.1016/j.molstruc.2021.130230

Cited by 5 publications

(2 citation statements)

References 46 publications

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“…Although in silico studies in the context of the impact of the rs4646994 polymorphism on treatment with ACEi drugs have already been conducted, their main target was usually captopril or lisinopril [44,45]. In this study, the interactions between two ACE domains and four drugs that are registered in Poland as those that can be used in the treatment of diabetic nephropathy [46] were taken into account.…”

Section: Discussionmentioning

confidence: 99%

The Role of Angiotensin-Converting Enzyme (ACE) Polymorphisms in the Risk of Development and Treatment of Diabetic Nephropathy

Król-Kulikowska,

Abramenko,

Jakubek

et al. 2024

JCM

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Background: Angiotensin-converting enzyme (ACE) is responsible for the production of angiotensin II, and increased production of angiotensin II is observed in diabetes. What is more, ACE polymorphisms may play a role in the development of diabetic nephropathy. The aim of this study was to assess the role of selected ACE polymorphisms (rs4343 and rs4646994) in the risk of development of diabetic nephropathy and in the likelihood of renal replacement therapy. Methods: ACE polymorphisms were analyzed in a group of 225 patients who were divided into three subgroups. The rs4343 polymorphism was determined using the PCR-RFLP, and the rs4646994 polymorphism was determined using the PCR. Molecular docking between domains of ACE and its ligands was performed by using AutoDock Vina. Results: The G/G genotype of rs4343 polymorphism is associated with increased odds of developing diabetic nephropathy. The G allele is also associated with a higher risk of this disease. Similar results were obtained in patients who had already had a kidney transplant as a result of diabetic nephropathy. Conclusions: The presence of G/G and G/A genotypes, and the G allele increases the likelihood of developing diabetic nephropathy. This may also be a risk factor for renal replacement therapy.

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Section: Discussionmentioning

confidence: 99%

The Role of Angiotensin-Converting Enzyme (ACE) Polymorphisms in the Risk of Development and Treatment of Diabetic Nephropathy

Król-Kulikowska,

Abramenko,

Jakubek

et al. 2024

JCM

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“…Five compounds exhibited potent inhibitory activity comparable to Captopril drug. Interestingly, glutarimide 19 revealed the most active ACE inhibitor displaying an IC 50 value of F I G U R E 2 Dose-dependent ACE inhibition activity of tested δ-lactams and glutarimides T A B L E 1 IC 50 values of active compounds and standard drug [19] Compound IC 50 (mg/ml) All starting materials were obtained from commercial suppliers and used without purification. NMR spectra were recorded on a 300 MHz Brucker spectrometer.…”

Section: Discussionmentioning

confidence: 99%

Synthesis and evaluation of new phosphonated δ‐lactam and glutarimide derivatives as angiotensin converting enzyme inhibitors

Abdelli

Bejaoui

Bougatef

et al. 2022

Journal of Heterocyclic Chem

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An efficient synthesis of new γ,δ‐insaturated δ‐lactam and glutarimide derivatives bearing a phosphonomethyl group from a common allylphosphonate precursor is described. Our approach is based on a two‐step procedure involving the preparation of phosphonated‐1,5‐ketoester and −1,5‐diester followed by an amidation–heterocyclization sequence. The first step proceeds via Michael's addition of ethyl acetoacetate and diethyl malonate on an allylphosphonate starting material. The second step consists of a base‐promoted intramolecular amidation‐cyclization sequence with primary amines, which accounts for the construction of δ‐lactams and glutarimide skeletons. We performed the evaluation of angiotensin I‐converting enzyme (ACE) inhibition using an in vitro enzyme assay on six new compounds. Five compounds showed potent ACE inhibitory activity, with IC50 values ranging from 0.02 to 0.27 mg/ml. Compared with Captopril, used as a reference drug, two new glutarimide derivatives exhibited higher efficiency ACE inhibition activity.

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Towards effective antimicrobial agents: tailoring metal complexes derived acetyl acetone-4-imino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 2-aminothiazole schiff base

Selvan,

Ramachandran,

Cyril

et al. 2024

Discov. Chem.

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Synthesis, crystal structure, molecular docking studies and biological evaluation of aryl substituted dihydroisoquinoline imines as a potent angiotensin converting enzyme inhibitor

Cited by 5 publications

References 46 publications

The Role of Angiotensin-Converting Enzyme (ACE) Polymorphisms in the Risk of Development and Treatment of Diabetic Nephropathy

The Role of Angiotensin-Converting Enzyme (ACE) Polymorphisms in the Risk of Development and Treatment of Diabetic Nephropathy

Synthesis and evaluation of new phosphonated δ‐lactam and glutarimide derivatives as angiotensin converting enzyme inhibitors

Towards effective antimicrobial agents: tailoring metal complexes derived acetyl acetone-4-imino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 2-aminothiazole schiff base

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