The use of the docking studies with the purpose of searching Potential Antihypertensive Drugs

Drapak, Іryna; Suleiman, Marharyta M.; Protopopov, M. V.; Yeromina, H. O.; Ieromina, Z. G.; Sych, Irina; Perekhoda, Lina

doi:10.5958/0974-360x.2019.00846.1

Cited by 8 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Their effects are greater than expected by their ability to lower blood pressure alone. Although significant advances have been made in the therapeutic blockade of the renin-angiotensin-aldosterone system (RAAS or RAS), the use of angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers and non-selective aldosterone receptor antagonists, there is a clear need for both additional blocking strategies and enhancements of the current therapeutic approaches [21].…”

Section: Resultsmentioning

confidence: 99%

The Synthesis and In Silico Antihypertensive Activity Prognosis of New Mannich Bases Containing the 1,2,4-Triazole Moiety

Perekhoda¹,

Georgiyants²,

Yeromina³

et al. 2020

Ch&Cht

View full text Add to dashboard Cite

As a part of our continuous research on potential antihypertensive agents among morpholine and piperidine derivatives, 10 novel target compounds containing 1,2,4-triazole and morpholine or piperidine moieties have been designed and synthesized, and the docking studies have been conducted in order to find biologically active substances with the antihypertensive activity. The in silico studies have shown that all compounds synthesized are promising angiotensin converting enzyme inhibitors and belong to the toxicity class 4 and 5 according to the classification of chemicals by the OECD project.

show abstract

Section: Resultsmentioning

confidence: 99%

The Synthesis and In Silico Antihypertensive Activity Prognosis of New Mannich Bases Containing the 1,2,4-Triazole Moiety

Perekhoda¹,

Georgiyants²,

Yeromina³

et al. 2020

Ch&Cht

View full text Add to dashboard Cite

show abstract

“…Being mesoionic compounds, thiadiazoles can easily penetrate cell membranes. The thiadiazole containing compounds exhibited a wide range of activities (anti-inflammatory, antibacterial, antifungal, antiviral, cardioprotective, and an tidiabetic) [11][12][13][14][15][16]. It was reported the anti cancer activity of thiadiazole derivatives [17][18][19][20].…”

Section: Introductionmentioning

confidence: 99%

Study of the anticancer activity of N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide toward human tumor cells in vitro

et al. 2023

View full text Add to dashboard Cite

In vitro study and characterization of anticancer activity of new heterocyclic derivati ve -N(5methyl [1,3,4]thiadiazol2yl)propionamide. Methods. The cell culture; MTT assay. Results. We synthesized N(5methyl[1,3,4]thiadiazol2yl)propionamide, which possessed diuretic, cardioprotective, and anti-inflammatory effects. Here, we investigated its cytotoxi ci ty effect towards the tumor cell lines of various tissue origins: liver (HepG2), breast (MCF7), lung (A549), cervical (KB31), and leukemia (HL60) cells, as well as towards the non-tumor cells (НЕК293 and NIH3T3). The IC 50 values of the synthesized compound for tumor cells were in the range of 9.4-97.6 μg/mL. We found that the human hepatocellular carcinoma HepG2 cells were the most sensitive to the action of N(5methyl[1,3,4]thiadiazol 2yl)propionamide with the IC 50 value of 9.4 μg/mL. The studied derivative slightly inhibited the growth of the pseudonormal HEK293 and NIH3T3 cells. Conclusions. The antipro li fe rative activity of N(5methyl[1,3,4]thiadiazol2yl)propionamide dropped in the order: hepatocarcinoma > leukemia > breast carcinoma cells. Thus, we revealed in the molecule of N(5methyl[1,3,4]thiadiazol2yl)propionamide a combination of the diuretic, cardioprotec tive, anti-inflammatory and anticancer activities, which is of great significance for this agent as a potent anticancer medicine. K e y w o r d s: N(5methyl[1,3,4]thiadiazol2yl)propionamide, cytotoxicity in vitro, anti cancer activity.

show abstract

“…The use of various substituents in the thiazole fragment gives new biologically active compounds. [5][6] Thiazole derivatives exhibit a wide range of biological properties and are important reagents. Some of them such as Troglitazone, Rosiglitazone, Pioglitazone, Teneligliptin are widely used in the treatment of type 2 diabetes T2D.…”

Section: Introductionmentioning

confidence: 99%

Fructose Transformation into 5-Hydroxymethylfurfural over Natural Transcarpathian Zeolites

Patrylak¹,

Коновалов²,

Yakovenko³

et al. 2022

ChChT

View full text Add to dashboard Cite

Based on Transcarpathian zeolite the catalysts in calcium-lanthanum-ammonium form were synthesized and modified by steaming and dealumination with ethylenediaminetetraacetic acid. The samples were characterized by using nitrogen adsorption/desorption, XRD, XRF, and FTIR-spectroscopy. The yield of 5 hydroxymethylfurfural over modified samples at 433 K was found to be 50 and 83% at a practically full conversion of fructose.

show abstract

The use of the docking studies with the purpose of searching Potential Antihypertensive Drugs

Cited by 8 publications

References 0 publications

The Synthesis and In Silico Antihypertensive Activity Prognosis of New Mannich Bases Containing the 1,2,4-Triazole Moiety

The Synthesis and In Silico Antihypertensive Activity Prognosis of New Mannich Bases Containing the 1,2,4-Triazole Moiety

Study of the anticancer activity of N-(5-methyl-[1,3,4]thiadiazol-2-yl)-propionamide toward human tumor cells in vitro

Fructose Transformation into 5-Hydroxymethylfurfural over Natural Transcarpathian Zeolites

Contact Info

Product

Resources

About