Design, synthesis, and AChE inhibitory activity of new benzothiazole–piperazines

Özkay, Ümide Demir; Can, Özgür Devrim; Sağlık, Begüm Nurpelin; Çevik, Ulviye Acar; Levent, Serkan; Özkay, Yusuf; Ilgın, Sinem; Atlı, Özlem

doi:10.1016/j.bmcl.2016.10.041

Cited by 83 publications

(67 citation statements)

References 60 publications

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“…A novel series of benzothiazole‐piperazine compounds were designed and synthesized as potential acetylcholine esterase (AChE) inhibitors by Demir et al The inhibitory potential of the compounds on AChE was investigated. Among the compounds, 49a and 49b exhibited very good activity on AChE enzyme.…”

Section: Biological Applications Of Benzothiazole Derivativesmentioning

confidence: 99%

Therapeutic advancement of benzothiazole derivatives in the last decennial period

Tariq

Kamboj

Amir

2018

Arch. Pharm. Chem. Life Sci.

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Benzothiazole, a fused heterocyclic moiety, has attracted synthetic and medicinal chemists for good reasons. It is a valuable scaffold that possesses diverse biological activities, such as anticancer, anti-inflammatory, antimicrobial, antiviral, antimalarial, and anticonvulsant effects. This review mainly focusses on the recent research work on the different biological activities of benzothiazole-based compounds.

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Section: Biological Applications Of Benzothiazole Derivativesmentioning

confidence: 99%

Therapeutic advancement of benzothiazole derivatives in the last decennial period

Tariq

Kamboj

Amir

2018

Arch. Pharm. Chem. Life Sci.

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“…The cells were incubated as reported in the supplier's guide. The MTT assay was applied according to our previous studies [32][33][34]. The IC 50 values of compounds i and s were calculated from the plots of cell proliferation against concentrations by applying regression analyses on GraphPad Prism Version 5.…”

Section: Cytotoxicity Testmentioning

confidence: 99%

Synthesis, Molecular Docking Studies, and Antifungal Activity Evaluation of New Benzimidazole-Triazoles as Potential Lanosterol 14α-Demethylase Inhibitors

Can

Çevik

Sağlık

et al. 2017

Journal of Chemistry

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Due to anticandidal importance of azole compounds, a new series of benzimidazole-triazole derivatives ( a-s) were designed and synthesized as ergosterol inhibitors. The chemical structures of the target compounds were characterized by spectroscopic methods. The final compounds were screened for antifungal activity against Candida glabrata (ATCC 90030), Candida krusei (ATCC 6258), Candida parapsilosis (ATCC 22019), and Candida albicans (ATCC 24433). Compounds i and s exhibited significant inhibitory activity against Candida strains with MIC 50 values ranging from 0.78 to 1.56 g/mL. Cytotoxicity results revealed that IC 50 values of compounds i and s against NIH/3T3 are significantly higher than their MIC 50 values. Effect of the compounds i and s against ergosterol biosynthesis was determined by LC-MS-MS analysis. Both compounds caused a significant decrease in the ergosterol level. The molecular docking studies were performed to investigate the interaction modes between the compounds and active site of lanosterol 14--demethylase (CYP51), which is as a target enzyme for anticandidal azoles. Theoretical ADME predictions were also calculated for final compounds.

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“…The genotoxicity of the most effective compounds was determined by Ames assay using Ames MPF 98/100 mutagenicity assay sample kit (Xenometrix AG, Switzerland) as previously described . Salmonella typhimurium strains, TA98 (frameshift mutations) and TA100 (base‐pair substitutions), are used in this assay.…”

Section: Methodsmentioning

confidence: 99%

Design and evaluation of biological activities of 1,3‐oxazolidinone derivatives bearing amide, sulfonamide, and thiourea moieties

Karaman

Zainel

Kapkac

et al. 2018

Archiv der Pharmazie

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1,3-Oxazolidine-2-one is an important heterocyclic ring participating in the chemical structure of many drugs. In this research, 22 new amide/sulfonamide/thiourea derivatives (1-22) were obtained by the reaction of (S)-4-(4-aminobenzyl)-2(1H)-1,3-oxazolidinone with 4-substituted benzoyl chlorides, 4-substituted benzene sulfonyl chlorides, and 4-substituted phenyl isothiocyanates. The structures of all synthesized compounds were clarified by FT-IR, NMR, and mass spectroscopic and elemental analysis techniques. The synthesized compounds were screened for their antimicrobial activity. Antimicrobial susceptibility and cellular physiology were evaluated using the microbroth dilution assay and the flow cytometry method. As a result, it was determined that compound 16 displayed better antimicrobial activity than chloramphenicol against Gram-positive bacteria, especially Staphylococcus aureus. In order to understand the mechanism of effect of the compounds on the cell membrane, fluorescence microscopy was used. Cell membrane damage of the Gram positive bacteria treated with compound 16 was observed as a result of intense staining with propidium iodide. In addition, genotoxicity, cytotoxicity, and absorption, distribution, metabolism, and excretion (ADME) parameters of compound 16 were examined and it was found as non-mutagenic and non-cytotoxic at the concentration at which it showed antimicrobial activity. According to the calculated ADME parameters and drug likeness scores, the compounds can be good drug candidates, especially compound 16.

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Design, synthesis, and AChE inhibitory activity of new benzothiazole–piperazines

Cited by 83 publications

References 60 publications

Therapeutic advancement of benzothiazole derivatives in the last decennial period

Therapeutic advancement of benzothiazole derivatives in the last decennial period

Synthesis, Molecular Docking Studies, and Antifungal Activity Evaluation of New Benzimidazole-Triazoles as Potential Lanosterol 14α-Demethylase Inhibitors

Design and evaluation of biological activities of 1,3‐oxazolidinone derivatives bearing amide, sulfonamide, and thiourea moieties

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