Benzimidazoles in Drug Discovery: A Patent Review

Law, Christine S.; Yoon, Yeong Keng

doi:10.1002/cmdc.202100004

Cited by 52 publications

(24 citation statements)

References 104 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As a result of this review, researchers will be able to develop newer benzimidazole entities that target numerous enzymes and receptors for successful cancer treatment (Purushottamachar et al, 2019). Several benzimidazole derivatives were patented to date, and a few of their examples for different target proteins in cancer treatment are shown in Table 1 (Law & Yeong, 2021).…”

Section: Introductionmentioning

confidence: 99%

Recent advances of benzimidazole as anticancer agents

et al. 2023

View full text Add to dashboard Cite

Cancer is the second leading cause of death globally, with 9.6 million deaths yearly. As a life-threatening disease, it necessitates the emergence of new therapies. Resistance to current chemotherapies drives scientists to develop new medications that will eventually be accessible. Because heterocycles are so common in biological substances, compounds play a big part in the variety of medications that have been developed. The "Master Key" is the benzimidazole nucleus, which consists of a six-membered benzene ring fused with a five-membered imidazole/ imidazoline ring, which is an azapyrrole. One of the five-membered aromatic nitrogen heterocycles identified in American therapies that have been approved by the Food and Drug Administration (FDA). Our results show that benzimidazole's broad therapeutic spectrum is due to its structural isosteres with purine, which improves hydrogen bonding, electrostatic interactions with topoisomerase complexes, intercalation with DNA, and other functions. It also enhances protein and nucleic acid inhibition, tubulin microtubule degeneration, apoptosis, DNA fragmentation, and other functions. Additionally, readers for designing the more recent benzimidazole analogues as prospective cancer treatments.

show abstract

Section: Introductionmentioning

confidence: 99%

Recent advances of benzimidazole as anticancer agents

et al. 2023

View full text Add to dashboard Cite

show abstract

“…The research on benzimidazole chemistry goes back over a century. − Benzimidazole has gained considerable attention in medicinal and pharmaceutical chemistry . BzIm derivatives interact with the biopolymers of the living system such as proteins, enzymes, and receptors and are frequently used in the development of new therapeutic agents against multiple diseases. − The benzimidazole scaffold has also been reported as an organic corrosion inhibitor − for different metals in different media and as a multifunctional unit in heteroaromatic molecular systems for optoelectronics, nonlinear optics, photovoltaics, optical sensing, and bioimaging . The structural and spectroscopic features of BzIm are well established.…”

Section: Introductionmentioning

confidence: 99%

Dual Photochemistry of Benzimidazole

et al. 2023

View full text Add to dashboard Cite

Monomers of benzimidazole trapped in an argon matrix at 15 K were characterized by vibrational spectroscopy and identified as 1H-tautomers exclusively. The photochemistry of matrix-isolated 1H-benzimidazole was induced by excitations with a frequency-tunable narrowband UV light and followed spectroscopically. Hitherto unobserved photoproducts were identified as 4H- and 6H-tautomers. Simultaneously, a family of photoproducts bearing the isocyano moiety was identified. Thereby, the photochemistry of benzimidazole was hypothesized to follow two reaction pathways: the fixed-ring and the ring-opening isomerizations. The former reaction channel results in the cleavage of the NH bond and formation of a benzimidazolyl radical and an H-atom. The latter reaction channel involves the cleavage of the five-membered ring and concomitant shift of the H-atom from the CH bond of the imidazole moiety to the neighboring NH group, leading to 2-isocyanoaniline and subsequently to the isocyanoanilinyl radical. The mechanistic analysis of the observed photochemistry suggests that detached H-atoms, in both cases, recombine with the benzimidazolyl or isocyanoanilinyl radicals, predominantly at the positions with the largest spin density (revealed using the natural bond analysis computations). The photochemistry of benzimidazole therefore occupies an intermediate position between the earlier studied prototype cases of indole and benzoxazole, which exhibit exclusively the fixed-ring and the ring-opening photochemistries, respectively.

show abstract

“…), proton pump inhibitor (omeprazole, lansoprazole, pantoprazole, rabeprazole, and tenatoprazole etc.) (Law & Yeong, 2021).…”

Section: Introductionmentioning

confidence: 99%

Density Functional Theory and Molecular Docking Analysis of Newly Synthesized and Characterized Benzimidazolium Salts

Üstün

Şahin

2022

Ordu Üniversitesi Bilim Ve Teknoloji Dergisi

View full text Add to dashboard Cite

N-heterosiklik karbenler ailesinin önemli bir üyesi olan benzimidazoller, farmasötik aktivitelerinin yanı sıra katalitik özellikleri ile de dikkat çekmektedir. Bu moleküllerin sentezlenmesi ve türevlendirilmesi nispeten kolay olduğundan, bu bileşikler istenen özelliklere sahip yeni türlerin ve bu türlerin metal komplekslerinin sentezinde sıklıkla kullanılırlar. Bu tür farmasötik moleküllerin doku ve kan bileşenleri ile etkileşimleri önemlidir. Biyoaktif türlerin kandaki en önemli proteinlerden biri olan serum albümini ile etkileşimi sıkça çalışılan bir konudur ve bu araştırmalarda Sığır Serum Albümin sıklıkla kullanılmaktadır. In-siliko yöntemler birçok avantaj sağlar ve deneysel prosedürlerden önce önemli bilgiler verir. Bu çalışmada iki yeni benzimidazolyum tuzu sentezlenmiş ve karakterize edilmiştir. Moleküllerin yapısal analizi DFT tabanlı hesaplama yöntemleri ile analiz edildikten sonra, Global Reaktivite Tanımlayıcıları ile moleküllerin reaktiviteleri de incelenmiştir. Ayrıca moleküllerin Sığır Serum Albümin ile etkileşimleri moleküler doking yöntemleri ile analiz edildi.

show abstract

Benzimidazoles in Drug Discovery: A Patent Review

Cited by 52 publications

References 104 publications

Recent advances of benzimidazole as anticancer agents

Recent advances of benzimidazole as anticancer agents

Dual Photochemistry of Benzimidazole

Density Functional Theory and Molecular Docking Analysis of Newly Synthesized and Characterized Benzimidazolium Salts

Contact Info

Product

Resources

About