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Benzimidazoles in Drug Discovery: A Patent Review

Law CSW, Yeong KY

ChemMedChem, 2021 06 17;16(12):1861-1877.
PMID: 33646618 DOI: 10.1002/cmdc.202100004

Benzimidazole is a heterocyclic ring system that has been widely studied in the pharmaceutical field. For the past decade, numerous benzimidazole derivatives have been synthesized and evaluated for their wide range of pharmacological activities, which are beneficial for drug development. This article presents the biological effects of benzimidazole derivatives in each invention from 2015 to 2020. Two patent databases, Google Patents and Lens, were used to locate relevant granted patent applications. Specifically, this review delineates the role of patented benzimidazoles from a disease-centric perspective and examines the mechanisms of action of these compounds in related diseases. Most of the benzimidazoles have shown good activities against various target proteins. Whilst several of them have progressed into clinical trials, most patents presented novel therapeutic approaches for respective target diseases. Hence, their potential in being developed into clinical drugs are also discussed.
Synthesis, Molecular Docking, and Biological Evaluation of Benzimidazole Derivatives as Selective Butyrylcholinesterase Inhibitors

Ha ZY, Ong HC, Oo CW, Yeong KY

Curr Alzheimer Res, 2020;17(13):1177-1185.
PMID: 33602088 DOI: 10.2174/1567205018666210218151228

BACKGROUND: Benzimidazole is an interesting pharmacophore which has been extensively studied in medicinal chemistry due to its high affinity towards various enzymes and receptors. Its derivatives have been previously shown to possess a wide range of biological activities including anthelmintic, antihypertensive, antiulcer, as well as anticholinesterase activity.
OBJECTIVE: The objective of this study is to search for more potent benzimidazole-based cholinesterase inhibitors, through the modification of the 1- and 2-positions of the benzimidazole core.
METHODS: Synthesis of compounds were carried out via a 4-step reaction scheme following a previously reported protocol. Structure-activity relationship of the compounds are established through in vitro cholinesterase assays and in silico docking studies. Furthermore, cytotoxicity and blood brain barrier (BBB) permeability of the compounds were also investigated.
RESULTS: Among the synthesised compounds, three of them (5IIa, 5IIb, and 5IIc) exhibited potent selective butyrylcholinesterase inhibition at low micromolar level. The compounds did not show any significant cytotoxicity when tested against a panel of human cell lines. Moreover, the most active compound, 5IIc, was highly permeable across the blood brain barrier.
CONCLUSION: In total 10 benzimidazole derivatives were synthesized and screened for their AChE and BuChE inhibitory activities. Lead compound 5Iic, represents a valuable compound for further development as potential AD therapeutics.
Fulltext Retropharyngeal abscess - A complication of laryngeal mask airway

Lynn E, Ping T, Keng Y, Singh R, Kwong W, Soon T, et al.

J Surg Case Rep, 2012 Oct 01;2012(10):7.
PMID: 24960747 DOI: 10.1093/jscr/2012.10.7

Retropharyngeal or parapharyngeal abscesses developing after intubation are rare. This can present as surgical emergency post extubation. We report a case of retropharyngeal abscess that probably occurred as a complication of laryngeal mask insertion.
Bibliometric analysis of the research landscape on rice husks gasification (1995-2019)

Nyakuma BB, Wong S, Mong GR, Utume LN, Oladokun O, Wong KY, et al.

Environ Sci Pollut Res Int, 2021 Sep;28(36):49467-49490.
PMID: 34355317 DOI: 10.1007/s11356-021-15761-x

The processing of rice (Oryza sativa L.) generates large quantities of lignocellulosic wastes termed rice husks (RH). Numerous researchers have proposed biomass gasification as the panacea to the waste disposal and management challenges posed by RH. However, a comprehensive analysis of RH gasification is required to examine the research landscape and future directions on the area. The research landscape and global developments on RH gasification from 1995 to 2019 are examined through bibliometric analysis of 228 publications extracted from the Web of Science. Bioresource Technology is considered the most influential journal on the topic, whereas China is the most productive nation due to government policies and research funding. The most productive organization is the Harbin Institute of Technology, which is due to the significant contributions of Zhao YiJun and co-workers. Keyword analysis revealed three crucial research themes: gasification, biomass, and rice husks. The literature revealed that the syngas yield, distribution, and performance of RH gasification are significantly influenced by temperature, equivalence ratio, selected reactor, and gasifying medium. The techno-economic analysis of RH gasification revealed that government interventions such as high sales rates and low investment costs could enhance the commercial viability of the technology. Furthermore, the integration of RH gasification with carbon capture utilization and storage could promote the decarbonization of power plants, negative emissions, and net-zero climate goals. Overall, the paper provides valuable information for future researchers to identify strategic collaborators, journal publications, and research frontiers yet unexplored.