Structure-activity relationship of three synthesized benzimidazole-based oligosaccharides in human platelet activation

Chang, Yi; Hsu, Wen Hsien; Yang, Wen Bin; Jayakumar, Thanasekaran; Lee, Tzu Yin; Sheu, Joen Rong; Lu, Wan-Jung; Li, Jiun Yi

doi:10.3892/ijmm.2017.3133

Cited by 3 publications

(1 citation statement)

References 36 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Change et al ( Chang et al, 2017 ) investigated the antiplatelet activity of some novel saccharide-based benzimidazole derivatives. Compound 527 exhibited concentration-dependent inhibitory property against thrombin (0.01 U/ml) and collagen (1 µg/ml)-induced human platelet aggregation in an in vitro model.…”

Section: Biological Activitiesmentioning

confidence: 99%

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

et al. 2021

View full text Add to dashboard Cite

Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world’s most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.

show abstract

Section: Biological Activitiesmentioning

confidence: 99%

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

et al. 2021

View full text Add to dashboard Cite

show abstract

Synthesis, structural study and antitumor activity of novel alditol-based imidazophenanthrolines (aldo-IPs)

Gómez-Bra,

Gude,

Arias-Pérez

2024

Bioorganic & Medicinal Chemistry

View full text Add to dashboard Cite

Antiplatelet activity of new derivatives of benzimidazole containing sterically hindered phenolic group in their structure

Spasov¹,

Kucheryavenko²,

Gaidukova³

et al. 2020

RRP

View full text Add to dashboard Cite

Citation: Spasov AA, Kucheryavenko AF, Gaidukova KA, Kosolapov VA, Zhukovskaya ON (2020) Antiplatelet activity of new derivatives of benzimidazole containing sterically hindered phenolic group in their structure. Research Results in Pharmacology 6(1): 1-9. https://doi. AbstractIntroduction: Cardiovascular diseases are currently the leading cause of global disability and mortality. According to the centers for disease control and prevention, the average life expectancy of a person would be 10 years longer but for a high prevalence of cardiovascular diseases, and if antiplatelet drugs and special therapy were used. Materials and methods:Antiplatelet activity of the novel benzimidazole derivatives containing a sterically hindered phenolic group in their structure has been investigated in vitro, using a model of ADP-induced platelet aggregation of rabbit's plasma. The compounds exhibiting high antiplatelet activity and acetylsalicylic acid, as a reference drug, were examined for antioxidant properties in an ascorbate-dependent model of lipid peroxidation.Results: It was established that the compounds with high antiplatelet activity demonstrated the pronounced antioxidant action. The compound RU-1144 (1-(3,5-ditretbutyl-4-hydroxyphenyl) -1-hydroxypropyl)-phenyl-pyrimidobenzimidazole hydrochloride), in in vitro experiments, had a pronounced antiplatelet activity, surpassing the reference drug acetylsalicylic acid by 21.8 times; in the study of antioxidant activity, the leader compound was inferior to the reference drug dibunol by 1.7 times. By inhibiting intravascular platelet aggregation in vivo, this compound exceeded acetylsalicylic acid by 1.5 times and was slightly inferior to clopidogrel by 1.4 times. Discussion:Benzimidazole derivatives with a hindered phenolic substituent in their structure exhibited antiplatelet and antioxidant properties. It was established that the compounds with high antiplatelet activity demonstrated the pronounced antioxidant action. Conclusion:The chemical class of benzimidazole derivatives with a hindered phenolic substituent in their structure is promising for the search for new antiaggregant and antioxidant drugs.

show abstract

Structure-activity relationship of three synthesized benzimidazole-based oligosaccharides in human platelet activation

Cited by 3 publications

References 36 publications

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Synthesis, structural study and antitumor activity of novel alditol-based imidazophenanthrolines (aldo-IPs)

Antiplatelet activity of new derivatives of benzimidazole containing sterically hindered phenolic group in their structure

Contact Info

Product

Resources

About