scholarly journals Interaction of SARS-CoV-2 spike protein with angiotensin converting enzyme inhibitors and selected compounds from the chemical entities of biological interest

2021 ◽  
Vol 10 (1) ◽  
Author(s):  
Suleiman Aminu ◽  
Mohammed Auwal Ibrahim ◽  
Abdullahi Balarabe Sallau
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Initial Step ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Binding Energies ◽  
Spike Protein ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Discovery Studio

Abstract Background Recent COVID-19 outbreak has prompted the search of novel therapeutic agents to treat the disease. The initial step of the infection involves the binding of the virus through the viral spike protein with the host angiotensin converting enzyme 2 (ACE2). In this study, the interaction of some ACE or ACE2 inhibitors and their analogues as well as selected compounds with the viral spike protein as a strategy to hinder viral-ACE2 interaction were investigated. SARS-CoV-2 spike protein as well as the ligands were retrieved from protein databank and ChEBI database respectively. The molecules were prepared before initiating the virtual screening using PyRx software. Discovery studio was used to further visualize the binding interactions between the compounds and the protein. Results The ACE inhibitors and their analogues fosinopril (1-), fosinopril and moexipril have the best binding affinity to the protein with binding energies < − 7.0 kcal/mol while non-flavonoid stilben-4-ol binds with free binding energy of − 7.1 kcal/mol. Others compounds which belong to either the flavonoids, terpenes and alkaloid classes also have binding energies  < − 7.0 kcal/mol. Such high binding energies were enhanced via hydrogen bond (h-bond) interactions in addition to other interactions observed between the compounds and the amino acid residues of the protein. Conclusions The ACE inhibitors and their analogues as well as the selected compounds could serve as inhibitors of the spike protein as well as lead in drug discovery processes to target the SARS-CoV-2 virus.

scholarly journals Medicines in the rehabilitation of patients after myocardial infarction: angiotensin-converting enzyme inhibitors

2010 ◽  
Vol 1 (1) ◽  
pp. 62-64
Author(s):  
A. S Galyavich
Keyword(s):  
Myocardial Infarction ◽  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Ventricular Dysfunction ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Left Ventricular ◽  
Diabetic Patients ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors

The paper analyzes the use of angiotensin-converting enzyme (ACE) inhibitors in patients after prior myocardial infarction. It presents the data of controlled studies, which indicate that it is warranted to use ACE inhibitors to improve prognosis in patients. It is concluded that it is unreasonable for a physician not to prescribe ACE inhibitors to post-myocardial infarction patients with obvious or asymptomatic left ventricular dysfunction and to diabetic patients (if no contraindications).

Free radical scavenging: a potentially beneficial action of thiol-containing angiotensin converting enzyme inhibitors

1990 ◽  
Vol 18 (6) ◽  
pp. 1184-1185 ◽  
Author(s):  
MRIDULA CHOPRA ◽  
JOHN McMURRAY ◽  
JENNIFER STEWART ◽  
HENRY J. DARGIE ◽  
W. EWEN SMITH
Keyword(s):  
Free Radical ◽  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Radical Scavenging ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Converting Enzyme ◽  
Ischaemia Reperfusion Injury ◽  
Converting Enzyme Inhibitors ◽  
Beneficial Action

Summary Free radical (FR) scavenging may be a therapeutically useful adjunctive property of angiotensin converting enzyme (ACE) inhibitors. In this study we have shown that SH-containing ACE inhibitors (captopril, epicaptopril, zofenopril) are potent FR scavengers at a concentration of 4 × 10-5m whereas non-SH ACE inhibitors (enalaprilat, quinaprilat and perindoprilat) have no FR-scavenging activity at this concentration. Furthermore, the SH-containing agents preferentially scavenged general radicals rather than superoxide radicals, i.e. suggesting that these drugs would be effective in quenching the culprit FR in ischaemia/reperfusion injury.

scholarly journals A REVIEW ON ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF CALCIUM CHANNEL BLOCKERS AND ANGIOTENSIN- CONVERTING ENZYME INHIBITORS IN BULK AND PHARMACETICAL FORMULATION

2019 ◽  
Vol 7 (4) ◽  
Author(s):  
Gawade Sonba. C ◽  
G.K. Dyade ◽  
Dr.S.G. Jadhav
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Channel Blockers ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Limit Of Quantitation

A simple, economical and rapid by UV detector and PDA Detector was used for Estimation of Trandolapril and Verapamil in combination and other drugs in various Pharmaceutical formulation. Calcium channel blockers(CCBs) and angiotensin- converting enzyme (ACE) inhibitors  has been developed and fully validated by High performance liquid Chromatographic Methods. Calcium channel blockers (CCBs) or Calcium antagonists are among the most widely used drugs in cardiovascular medicine and hypertension also in angina. CCBs promote vasodilator activity by reducing calcium influx into vascular smooth muscle cells by interfering with calcium channels in the cell membrane. Trandolapril is a potent nonsulfhydryl and dicarboxyl containing Angiotensin converting inhibitor (ACE). Trandolapril used to treatment of hypertension appears to result the inhibition of tissue ACE activity and to improve survival myocardial infarction thereby reduce angiotensin II formation. It includes drugs like Trandolapril, Norverapamil, Nifedipine, Verapamil. This Review enlists different method Developed, Validated and determination of Calcium channel blockers and angiotensin- converting enzyme inhibitors Like, RP-HPLC, LC-MS/MS and HPLC UV- Spectophotometric method. This method was also validated for various validation terms indicates that precise, accurate, linearly, and limit of Detection and limit of Quantitation as per ICH guidelines. Keywords: HPLC Chromatography, Calcium Channel blocker, angiotensin- converting enzyme (ACE) inhibitors, Hypertension, Validation etc.

scholarly journals ANALYSIS OF APPROACHES TO THE DEVELOPMENT AND VALIDATION OF THE METHODS OF ANALYSIS OF SOME ACTIVE PHARMACEUTICAL INGREDIENTS FROM THE GROUP OF ANGIOTENSIN CONVERTING ENZYME INHIBITORS IN DRUGS AND BIOLOGICAL LIQUIDS

2019 ◽  
pp. 1-7 ◽  
Author(s):  
Liliya Logoyda
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Method Development ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Literature Survey ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Methods Of Analysis ◽  
Biological Liquids

The quantity of medication brought into the marketplace is growing each year. Analytical method development is increasingly being introduced into fundamental pharmaceutical research and pharmaceutical analysis practice, taking into account their high sensitivity, accuracy, specificity and expressiveness. Search criteria was analytical method development for medicines from group of ACE inhibitors. Literature survey has been done in range of years 1990-2018 to make the review updated and comprehensive and to show the new approacheches to the development of the methods of analysis ACE inhibitors. The sources were world recognized journals and key words used as filter were angiotensin-converting enzyme inhibitors, captopril, enalapril, method development, spectrophotometry, HPLC, UHPLC. The current review is created with an intended to focus on the advantage of HPLC. Literature survey revealed that a number of methods have been reported for estimation of ACE inhibitors individually or in combination with other drugs. However, there is very few analytical methods reported for the simultaneous analysis of these drugs in a combined dosage formulation by HPLC. In additional, analysis of approaches to the development of the methods of analysis of ACE inhibitors in drugs and biological liquids has been shown that HPLC is the most suitable method for analyses ACE inhibitors in substances, drugs, biological liquids to performe routine analysis of medicines, pharmacokinetic (bioequivalence in vivo), dissolution test for final dosages forms (bioequivalence in vitro, biowaiver procedure).

scholarly journals POTENTIAL OF ANGIOTENSIN-CONVERTING ENZYME INHIBITORS IN THE TREATMENT OF PATIENTS WITH ARTERIAL HYPERTENSION AND CORONARY HEART DISEASE

2013 ◽  
Vol 12 (1) ◽  
pp. 80-87
Author(s):  
A. G. Evdokimova ◽  
V. V. Evdokimov
Keyword(s):  
Coronary Heart Disease ◽  
Heart Disease ◽  
Angiotensin Converting Enzyme ◽  
Arterial Hypertension ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Protective Effects ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors

For the last 30 years, angiotensin-converting enzyme (ACE) inhibitors have been playing a key role in the management of arterial hypertension (AH) and related cardiovascular disease. This review discusses the mechanisms of action and organo-protective effects of ACE inhibitors. Enalapril is the most extensively studied and widely used in the international clinical practice ACE inhibitor. The authors analyse the results of the studies on enalapril therapy in AH, coronary heart disease (CHD), chronic heart failure, metabolic syndrome, and postmenopause. It has been demonstrated that the combination antihypertensive therapy with a β-adrenoblocker nebivolol, enalapril, and hydrochlorothiazide (such as Berlipril® Plus) is safe and effective in patients with AH and CHD. 

scholarly journals Angiotensin converting enzyme inhibitors do not increase the risk of poor outcomes in COVID-19 disease. A multi-centre observational study

2020 ◽  
Vol 65 (4) ◽  
pp. 149-153 ◽  
Author(s):  
Khurram Shahzad Khan ◽  
Hamish Reed-Embleton ◽  
Jen Lewis ◽  
Pamela Bain ◽  
Sajid Mahmud
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Hospitalised Patients ◽  
Increased Risk ◽  
All Cause Mortality ◽  
Randomised Controlled

Background and aims Hypertension is associated with an increased risk of severe outcomes with COVID-19 disease. Angiotensin Converting Enzyme (ACE) inhibitors are widely used as a first line medication for the treatment of hypertension in the UK, although their use was suggested in early reports to increase the risk associated with SARS-CoV-2 infection. Methods A prospective cohort study of hospitalised patients with laboratory confirmed COVID-19 was conducted across three hospital sites with patients identified on the 9th April 2020. Demographic and other baseline data were extracted from electronic case records, and patients grouped depending on ACE inhibitor usage or not. The 60-day all-cause mortality and need for intubation compared. Results Of the 173 patients identified, 88 (50.8%) had hypertension. Of these 27 (30.7%) used ACE inhibitors. We did not find significant differences in 60-day all-cause mortality, the requirement for invasive ventilation or length of stay between our patient cohorts after adjusting for covariates. Conclusion This study contributes to the growing evidence supporting the continued use of ACE inhibitors in COVID-19 disease, although adequately powered randomised controlled trials will be needed to confirm effects.

Angiotensin Converting Enzyme Inhibitors May Cause Renal Impairment in Diabetes Mellitus

1988 ◽  
Vol 33 (2) ◽  
pp. 247-248 ◽  
Author(s):  
J. Webster ◽  
L.E. Murchison ◽  
O.J. Robb
Keyword(s):  
Diabetes Mellitus ◽  
Renal Function ◽  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Diabetic Patients ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Careful Investigation

Angiotensin converting enzyme (ACE) inhibitors have been recommended for the treatment of diabetic nephropathy. However, it should be remembered that diabetic patients may also develop atheromatous renal artery stenosis. In such patients ACE inhibitors may have adverse effects on renal function. Careful investigation and monitoring is essential when ACE inhibitors are used in diabetes.

Angioedema secondary to angiotensin-converting enzyme inhibitors

1994 ◽  
Vol 108 (8) ◽  
pp. 696-698 ◽  
Author(s):  
J. P. M. Pracy ◽  
J. A. McGlashan ◽  
R. M. Walsh ◽  
M. J. Gleeson
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Cardiac Failure ◽  
Ace Inhibitors ◽  
Side Effect ◽  
Enzyme Inhibitors ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Threatening Condition ◽  
Life Threatening

AbstractAngioedema secondary to angiotensin-converting enzyme (ACE) inhibitors is rare, but it is a side effect which is likely to be seen more frequently because of the increased use of these drugs to treat cardiac failure and hypertension. Presentation is variable and the diagnosis may go unrecognized for many months or years. The cases reported illustrate problems both in the diagnosis and management of this life-threatening condition.

A Survey of Current Use of Angiotensin-Converting-Enzyme Inhibitors by Scottish Physicians in the Treatment of Chronic Cardiac Failure

1989 ◽  
Vol 34 (2) ◽  
pp. 425-427 ◽  
Author(s):  
J. McMurray ◽  
C.C. Lang ◽  
D.D. Maclean ◽  
D.G. McDevitt ◽  
A.D. Struthers
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Ace Inhibitors ◽  
Enzyme Inhibitors ◽  
Cost Savings ◽  
Extended Period ◽  
Angiotensin Converting Enzyme Inhibitors ◽  
Initial Therapy ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
General Physicians

318 consultant physicians in Scotland were sent a questionnaire on their use of angiotensin converting enzyme (ACE) inhibitors to treat chronic heart failure (CHF). 229 (72%) replies were received. Of these 91% used ACE inhibitors for CHF; 22% were geriatricians, 58% general physicians and 20% cardiologists. All groups reserved ACE inhibitors for patients uncontrolled by diuretics alone. Compared to general physicians, cardiologists used ACE inhibitors in preference to other vasodilators and digoxin, used higher doses and commenced treatment more often on a day-patient basis. Cardiologists also commonly started treatment with captopril even if continuing with enalapril. Geriatricians used ACE inhibitors as frequently as cardiologists but at lower doses; they did not report side-effects more frequently. Further investigation of the safety and possible cost savings of supervised day-patient rather than in-patient, introduction of ACE inhibitors for CHF is now merited. To avoid an extended period of patient observation after the first dose of ACE inhibitor, captopril might also be given as the initial therapy, even if continuing with enalapril. This policy would also reduce the risk of any hypotensive response being prolonged.

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