Design, synthesis and biological evaluation of novel fluoro-substituted benzimidazole derivatives with anti-hypertension activities

Wu, Zhuo; Xia, Ming-Bao; Bertsetseg, D.; Wang, Yanhui; Bao, Xiaolu; Zhu, Weibo; Tao-Xu,; Chen, Pei-Ran; Tang, Hesheng; Yan, Yuan; Chen, Zhilong

doi:10.1016/j.bioorg.2020.104042

Cited by 28 publications

(20 citation statements)

References 17 publications

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“…A very recent report ( Yang et al, 2020 ) ascertained the promising pulmonary hypotensive effect of compound 399 with excellent pharmacokinetic profile in comparison with tadalafil. Finally, compounds 400–401 showed superior inhibition of AT1 receptor (IC 50 (mean ± SEM): 0.8 ± 0.1 and 2.3 ± 0.7, respectively) than the both standard losartan and telmisartan ( Wu et al, 2020 ).…”

Section: Biological Activitiesmentioning

confidence: 97%

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

et al. 2021

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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.

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Section: Biological Activitiesmentioning

confidence: 97%

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

et al. 2021

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“…Compound 64a further destabilized microtubules and accelerated depolymerization. A series of new fluoro-substituted benzimidazole hybrids were designed, synthesized and pharmacologically evaluated [ 69 ]. The new compounds were exposed to biological evaluation for their impacts on systolic blood pressure (SBP) and diastolic blood pressure (DBP) in spontaneously hypertensive rats.…”

Section: Five-membered Heterocyclic Compoundsmentioning

confidence: 99%

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

Ebenezer

Jordaan

Carena

et al. 2022

IJMS

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Heterocyclic compounds are a class of compounds of natural origin with favorable properties and hence have major pharmaceutical significance. They have an exceptional adroitness favoring their use as diverse smart biomimetics, in addition to possessing an active pharmacophore in a complex structure. This has made them an indispensable motif in the drug discovery field. Heterocyclic compounds are usually classified according to the ring size, type, and the number of heteroatoms present in the ring. Among different heterocyclic ring systems, nitrogen heterocyclic compounds are more abundant in nature. They also have considerable pharmacological significance. This review highlights recent pioneering studies in the biological assessment of nitrogen-containing compounds, namely: triazoles, tetrazoles, imidazole/benzimidazoles, pyrimidines, and quinolines. It explores publications between April 2020 and February 2022 and will benefit researchers in medicinal chemistry and pharmacology. The present work is organized based on the size of the heterocyclic ring.

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“…The unique structural features of benzimidazole and the wide range of biological activities of its derivatives make it preferred in drug discovery (Gaba et al, 2014). Introduced benzimidazole as the dominant skeleton is wildly used in drug design which can promote the biological activities, such as antiulcer anti‐inflammatory, anti‐hypertensive, anti‐tumor, antiviral, and antifungal (Azahar et al, 2019; Kale et al, 2016; Wu et al, 2020). Benzimidazole, as the one of the earliest nitrogen‐containing heterocyclic compounds ever found, has a flat ring system in which benzene rings are thickly combined on the 4, 5th position of the imidazole ring (Alzhrani et al, 2021).…”

Section: Introductionmentioning

confidence: 99%

Recent progress of research on anti‐tumor agents using benzimidazole as the structure unit

Peng

Chen

et al. 2022

Chem Biol Drug Des

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With the development of exploration for disease‐related proteins or receptors, more and more novel structural lead compounds are required to designed and synthesized. The benzimidazole is an effective structural unit in which the benzene ring is fused at the 4 and 5 positions of the imidazole ring and wildly used in drug design. Here, we introduce some recent progress of research for anti‐tumor agents which was target to various target proteins such as DNA topoisomerase, angiogenesis, serine/threonine protein kinase, and tyrosine protein kinase. These anti‐tumor agents are all introduced benzimidazole as the structure unit. Further docking study showed that the benzimidazole group was not only act as a skeleton to expand the structure of molecule but also as an excellent ligand unit to form hydrogen bond or π–π conjugation and hydrophobic interaction with target proteins or receptors. We expect that introducing benzimidazole in the chemical structure could be a reasonable and priority strategy in novel anti‐tumor agents' design.

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Design, synthesis and biological evaluation of novel fluoro-substituted benzimidazole derivatives with anti-hypertension activities

Cited by 28 publications

References 17 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

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

Recent progress of research on anti‐tumor agents using benzimidazole as the structure unit

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