1,2,4-Trisubstituted imidazolinones with dual carbonic anhydrase and p38 mitogen-activated protein kinase inhibitory activity

Georgey, Hanan H.; Manhi, Fatma M.; Mahmoud, Walaa R.; Mohamed, Nehad A.; Berrino, Emanuela

doi:10.1016/j.bioorg.2018.09.037

Cited by 14 publications

(17 citation statements)

References 23 publications

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“…In a study by Georgey et al, [ 66 ] various 1,2,4‐trisubstituted imidazoline‐5‐ones were investigated as CAIs. They reported that the compounds tested were ineffective inhibitors against hCA I with K i values in the range of 823 to >10,000 nM, whereas hCA II was inhibited by their compounds in the range of 5 to >10,000 nM.…”

Section: Resultsmentioning

confidence: 99%

“…The spectral and experimental data of the isolated open‐chain product 5 compounds are given below. [ 66 ]…”

Section: Methodsmentioning

confidence: 99%

“…Isolation and purification of the compounds 4a – e were carried out in a similar manner as for 3a – e and 5 . [ 66 ]…”

Section: Methodsmentioning

confidence: 99%

“…Several arylimidazoline benzenesulfonamide hybrids shown in Figure 2 were reported as useful CA inhibitors. [ 66 ] In another study, a series of sulfanilamide incorporating imidazol‐2(3 H )‐one/thiones scaffold was studied against CA I, II, IX, and XII isoenzymes. These compounds were not considered useful as CA I and II inhibitors, whereas they can be considered as CA IX and XII inhibitors.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and in vitro carbonic anhydrases and acetylcholinesterase inhibitory activities of novel imidazolinone‐based benzenesulfonamides

Tuğrak

Gül

Demir

et al. 2020

Archiv der Pharmazie

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New imidazolinone‐based benzenesulfonamides 3a–e and 4a–e were synthesized in three steps and their chemical structures were confirmed by 1H NMR (nuclear magnetic resonance), 13C NMR, and high‐resolution mass spectrometry. The benzenesulfonamides used were sulfacetamide (3a, 4a), sulfaguanidine (3b, 4b), sulfanilamide (3c, 4c), sulfadiazine (3d, 4d), sulfamerazine (3e), and sulfathiazole (4e). The compounds were evaluated against carbonic anhydrase (CA) and acetylcholinesterase (AChE) enzymes to obtain possible drug candidate/s. The lead compounds of the series were 3a and 4a against human CA (hCA) I, whereas 3d and 4a were leads against hCA II in terms of Ki values. Series 4 includes more effective CAs inhibitors than series 3 (except 3d). Series 4 compounds having a nitro group (except 4d) were 3.3–4.8 times more selective inhibitors than their corresponding analogues 3a–d in series 3, in which hydrogen was located in place of the nitro group, by considering Ki values against hCA II. Compounds 3c and 4c, where the sulfanilamide moiety is available, were the leads in terms of AChE inhibition with the lowest Ki values. The use of secondary sulfonamides was a more effective modification on CA inhibition, whereas the primary sulfonamide was the effective substitution in terms of AChE inhibitory potency.

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Section: Resultsmentioning

confidence: 99%

“…The spectral and experimental data of the isolated open‐chain product 5 compounds are given below. [ 66 ]…”

Section: Methodsmentioning

confidence: 99%

“…Isolation and purification of the compounds 4a – e were carried out in a similar manner as for 3a – e and 5 . [ 66 ]…”

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Synthesis and in vitro carbonic anhydrases and acetylcholinesterase inhibitory activities of novel imidazolinone‐based benzenesulfonamides

Tuğrak

Gül

Demir

et al. 2020

Archiv der Pharmazie

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“…Hence the researchers have utilized the above mentioned information in the design and development of drug compounds as enzyme inhibitors. This derivative work includes synthesis of many series of compounds possessing enzyme inhibitory properties [5,6]. Since diverse chemical pharmacores prevail that could inhibit various enzymes, the enzyme inhibitors are described in different classes depending upon the designed structural entity [7,8].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, pharmacological evaluation and structure-activity relationship of recently discovered enzyme antagonist azoles

Dorababu¹

2020

Heliyon

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Global people are suffering from the legion of diseases. Cytotoxic property of the chemical compound would not solely influence effective drug properties and reduce unnecessary side effects. Proteins/enzymes responsible for microbe proliferation or survival are specifically targeted and inhibited successfully making the cells to undergo apoptosis. Furthermore, isoforms of essential enzymes have distinct physiological functions; thereby inhibition of essential enzyme isoforms is an apt way to the clinical approach of disease neutralization. Drugs are designed so as to play significant roles such as signaling pathways in the oncogenic process including cell proliferation, invasion, and angiogenesis. The present review comprises collective information of the recent synthesis of various organic drug compounds in brief, which could inhibit particular enzyme. The review also covers the correlation of the structure of a drug molecule designed and its inhibitory activity. Also, the most significant enzyme inhibitors are highlighted and structural moieties/core units responsible for remarkable inhibitory values are emphasized.

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Synthesis, characterization, antioxidant power and acute toxicity of some new azo-benzamide and azo-imidazolone derivatives with in vivo and in vitro antimicrobial evaluation

Samad

Hawaiz

2019

Bioorganic Chemistry

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1,2,4-Trisubstituted imidazolinones with dual carbonic anhydrase and p38 mitogen-activated protein kinase inhibitory activity

Cited by 14 publications

References 23 publications

Synthesis and in vitro carbonic anhydrases and acetylcholinesterase inhibitory activities of novel imidazolinone‐based benzenesulfonamides

Synthesis and in vitro carbonic anhydrases and acetylcholinesterase inhibitory activities of novel imidazolinone‐based benzenesulfonamides

Synthesis, pharmacological evaluation and structure-activity relationship of recently discovered enzyme antagonist azoles

Synthesis, characterization, antioxidant power and acute toxicity of some new azo-benzamide and azo-imidazolone derivatives with in vivo and in vitro antimicrobial evaluation

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