Some pyrazoles derivatives: Potent carbonic anhydrase, α‐glycosidase, and cholinesterase enzymes inhibitors

Türkan, Fikret; Çetin, Adnan; Taslimi, Parham; Gülçın, İlhami

doi:10.1002/ardp.201800200

Cited by 70 publications

(43 citation statements)

References 50 publications

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“…It is found that the CS‐adsorbed PP film shows a new band at 1554 cm −1 corresponding to the NH bending vibration, which decreases when CS amino groups interact with the AgNP surface for the AgNP x /CS‐coated PP film. This behavior agrees with the fact that the coordination complex limits the NH vibrational mode and its intensity decreases . The surface functional groups of AgNP x /CS‐coated PP films were also analyzed from the absorbance band ratio from the amino to the methylene group (

A_{1556 {cm}^{- 1}} / A_{1456 {cm}^{- 1}}

).…”

Section: Resultssupporting

confidence: 76%

“…The antimicrobial activity can be imparted to materials employing compounds that reduce or inhibit the growth of microorganisms, without showing general toxicity in the surroundings of the treated center . The antibacterial agents (antibiotics) most commonly used come from completely natural products, such as aminoglycosides; chemically modified natural compounds, such as penicillin, cephalosporin, or carbapenem; and completely synthetic ones, such as sulfonamides . However, the widespread use of these substances and their abuse have led, in many cases, to bacterial resistance, a growing issue that calls for the development of new strategies .…”

Section: Introductionmentioning

confidence: 99%

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Original antifouling strategy: Polypropylene films modified with chitosan‐coated silver nanoparticles

Mosconi

Stragliotto

Slenk

et al. 2019

J of Applied Polymer Sci

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A new coating strategy of polypropylene (PP) films with silver nanoparticles (AgNPs) is proposed to obtain surfaces with antifouling properties. As a first step, the photograft polymerization is used to produce polyacrylic acid-grafted PP (PAA-grafted PP) films. A green AgNP synthesis is used by thermal reduction of AgNO 3 with amino groups of chitosan (CS), which controls ion diffusion and stabilizes nanoparticles. AgNP/CS complexes are adsorbed on PAA-grafted PP by electrostatic interactions, yielding AgNP/CS-coated PP films. These films show an excellent antimicrobial activity, even for AgNP contents as low as 0.08 wt %, reducing more than 4 log units in the viable Staphylococcus aureus concentration or inducing Escherichia coli death. This trend is consistent with an adequate amount of small AgNP adsorbed in an organized manner within a thin surface layer. Therefore, the antimicrobial activity of this film seems to be more than promising, used as an active surface for a wide range of applications.A suitable combination of a natural and a synthetic polymer improves the properties of the resulting material, which expands its application field. This methodology of synthesis has proved to be appropriate in areas such as biomedical materials, controlled Additional Supporting Information may be found in the online version of this article.

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A_{1556 {cm}^{- 1}} / A_{1456 {cm}^{- 1}}

).…”

Section: Resultssupporting

confidence: 76%

Section: Introductionmentioning

confidence: 99%

Original antifouling strategy: Polypropylene films modified with chitosan‐coated silver nanoparticles

Mosconi

Stragliotto

Slenk

et al. 2019

J of Applied Polymer Sci

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“…CA enzymes are classical which are inhibited by different compounds with a sulfonamide‐based (SO 2 NH 2 ) zinc‐binding group or their bioisosteres such as sulfamides and sulfamates. As CA II enzymes are the most physiologically plentiful isoforms, which they were mostly recorded as the predominant off‐purpose isozymes of which inhibitions were eschewed . Recently, multiple kinds of compounds have been searched as nonclassical CAIs, including polyamines, coumarins, phenols, carboxylic acids, fullerenes, and their derivatives …”

Section: Resultsmentioning

confidence: 99%

Synthesis, characterization, molecular docking and biological activities of novel pyrazoline derivatives

Türkan

Çetin

Taslimi

et al. 2019

Archiv der Pharmazie

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In this study, synthesis of ethyl 2-((4-bromophenyl)diazenyl)-3-oxo-phenylpropanoate 1 was carried out and a series of new 3H-pyrazol-3-ones (P1-7) were synthesized from 1 as well as various hydrazines. The obtained yields of the synthesized compounds were moderate (40-70%) and these compounds were confirmed by spectral data. These novel pyrazoline derivatives were effective inhibitor compounds of the human carbonic anhydrase I and II isozymes (hCAs I and II) and of the acetylcholinesterase (AChE) enzyme, with K i values in the range of 17.4-40.7 nM for hCA I, 16.1-55.2 nM for hCA II, and 48.2-84.1 nM for AChE. In silico studies were performed on the compounds inhibiting hCA I, hCA II, and AChE receptors. On the basis of the findings, the inhibition profile of the new pyrazoline compounds at the receptors was determined.

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“…[56,57] The influence of phenolic compounds on metabolic enzymes is at the last period and the results of the inhibition of phenolic compounds are found in the literature. [58][59][60][61]…”

Section: Discussionmentioning

confidence: 99%

Tannic acid as a natural antioxidant compound: Discovery of a potent metabolic enzyme inhibitor for a new therapeutic approach in diabetes and Alzheimer's disease

Türkan

Taslimi

Saltan

2019

J Biochem & Molecular Tox

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Multiple studies have been recorded on the synthesis and design of multi‐aim anti‐Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer's disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α‐glycosidase, α‐amylase, and butyrylcholinesterase (BChE). IC50 values of tannic acid obtained 11.9 nM against α‐glycosidase and 3.3 nM against α‐amylase, respectively. In contrast, Ki values were found of 50.96 ± 2.18 µM against AChE and 53.17 ± 4.47 µM against BChE. α‐Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level.

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Some pyrazoles derivatives: Potent carbonic anhydrase, α‐glycosidase, and cholinesterase enzymes inhibitors

Cited by 70 publications

References 50 publications

Original antifouling strategy: Polypropylene films modified with chitosan‐coated silver nanoparticles

Original antifouling strategy: Polypropylene films modified with chitosan‐coated silver nanoparticles

Synthesis, characterization, molecular docking and biological activities of novel pyrazoline derivatives

Tannic acid as a natural antioxidant compound: Discovery of a potent metabolic enzyme inhibitor for a new therapeutic approach in diabetes and Alzheimer's disease

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