Synthesis, biological evaluation, and bioinformatics analysis of indole analogs on AChE and GST activities

Çetin, Adnan; Toptas, Mesut; Türkan, Fikret

doi:10.1007/s00044-022-02974-z

Cited by 9 publications

(1 citation statement)

References 80 publications

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“…Among them, compound 48 was the most potent for AChE inhibitor with IC 50 value of 0.63 μM (Figure ). Structure–activity pattern suggested that substitution of methyl group at the para position of phenyl next to triazole nucleus was most desirable for inhibitory activity, whereas other substitution on phenyl ring or unsubstituted phenyl ring resulted in decreased activity . Inspired from the structure and activity profile of cymserine analogues, galantamine derivatives, thienothiazines, diarylimidazoles, N -(10)-substituted phenothiazine amide derivatives, and 1,5-benzothiazepines and isosorbide-2-carbamate esters, Jabeen et al rationally designed the 1,4-disubstituted-1,2,3-triazoles.…”

Section: 23-triazole Containing Derivatives For Development Of Anti-a...mentioning

confidence: 99%

Pathogenesis of Alzheimer’s Disease and Diversity of 1,2,3-Triazole Scaffold in Drug Development: Design Strategies, Structural Insights, and Therapeutic Potential

Singh,

Kaur

et al. 2023

ACS Chem. Neurosci.

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Alzheimer’s disease is a most prevalent form of dementia all around the globe and currently poses a significant challenge to the healthcare system. Currently available drugs only slow the progression of this disease rather than provide proper containment. Identification of multiple targets responsible for this disease in the last three decades established it as a multifactorial neurodegenerative disorder that needs novel multifunctional agents for its management and the possible reason for the failure of currently available single target clinical drugs. 1,2,3-Triazole is a miraculous nucleus in medicinal chemistry and the first choice for development of multifunctional hybrid molecules. Apart from that, it is an integral component of various drugs in clinical trials as well as in clinical practice. This review is focused on the pathogenesis of Alzheimer’s disease and 1,2,3-triazole containing derivatives developed in recent decades as potential anti-Alzheimer’s agents. The review will provide (A) precise insight of various established targets of Alzheimer’s disease including cholinergic, amyloid, tau, monoamine oxidases, glutamate, calcium, and reactive oxygen species hypothesis and (B) design hypothesis, structure–activity relationships, and pharmacological outcomes of 1,2,3-triazole containing multifunctional anti-Alzheimer’s agents. This review will provide a baseline for various research groups working on Alzheimer’s drug development in designing potent, safer, and effective multifunctional anti-Alzheimer’s candidates of the future.

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Section: 23-triazole Containing Derivatives For Development Of Anti-a...mentioning

confidence: 99%

Pathogenesis of Alzheimer’s Disease and Diversity of 1,2,3-Triazole Scaffold in Drug Development: Design Strategies, Structural Insights, and Therapeutic Potential

Singh,

Kaur

et al. 2023

ACS Chem. Neurosci.

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Synthesis and examination of 1,2,4‐triazine‐sulfonamide hybrids as potential inhibitory drugs: Inhibition effects on AChE and GST enzymes in silico and in vitro conditions

Rozbicki,

Oğuz,

Wolińska

et al. 2024

Archiv der Pharmazie

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The crucial functions of acetylcholinesterase (AChE) in neurotransmission and glutathione S‐transferase (GST) in detoxification and cellular protection underscore their pivotal roles as key enzymes, essential for maintaining the integrity of neurological and cellular homeostasis. For this purpose, a series of 1,2,4‐triazine‐sulfonamide hybrids (3a–r) was successfully synthesized, and subsequently evaluated for their inhibitory effects on AChE and GST. The investigation was complemented by molecular docking studies and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) predictions. The synthesized hybrids demonstrated significant promise in inhibiting both AChE and GST activities. Molecular docking analyses provided insights into the interactions between the compounds and the target enzymes, shedding light on potential binding modes and key amino acid residues involved. Furthermore, the study benefited from ADMET predictions, offering valuable information on the compounds' pharmacokinetic properties and potential toxicity. The promising results obtained from this comprehensive approach highlight the potential of these 1,2,4‐triazine‐sulfonamide hybrids as effective inhibitors of AChE and GST, paving the way for further development and optimization in the pursuit of novel therapeutic agents.

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Pharmacological assessment of disulfide–triazine hybrids: synthesis, enzyme inhibition, and molecular docking study

Türkan,

Cetin,

Rozbicki

et al. 2024

Med Chem Res

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Synthesis, biological evaluation, and bioinformatics analysis of indole analogs on AChE and GST activities

Cited by 9 publications

References 80 publications

Pathogenesis of Alzheimer’s Disease and Diversity of 1,2,3-Triazole Scaffold in Drug Development: Design Strategies, Structural Insights, and Therapeutic Potential

Pathogenesis of Alzheimer’s Disease and Diversity of 1,2,3-Triazole Scaffold in Drug Development: Design Strategies, Structural Insights, and Therapeutic Potential

Synthesis and examination of 1,2,4‐triazine‐sulfonamide hybrids as potential inhibitory drugs: Inhibition effects on AChE and GST enzymes in silico and in vitro conditions

Pharmacological assessment of disulfide–triazine hybrids: synthesis, enzyme inhibition, and molecular docking study

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