1-{[Dimethyl(phenyl)silyl]methyl}-3-(2-phenylethyl)-1 H -benzimidazol-3-ium bromide monohydrate (original) (raw)
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Crystal Structure and Pharmacological Importance of Benzimidazoles and Their Derivatives
BJSTR, 2017
Benzimidazoles and their derivatives exhibit a number of important pharmacological properties, such as antihistaminic [1], anti-ulcerative [2], anti allergic [3], and antipyretic [4]. In addition, benzimidazole derivatives are effective against the human cytomegalovirus (HCMV) [5] and are also efficient selective neuropeptide Y Y1 receptor antagonists [6]. We report here in the Crystal structure of 2-(4-(methylthio) phenyl)-1H-benzo[d] imidazole (1) and 2-(4-Methylsulfanylphenyl)-1Hbenzimidazol-3- ium bromide (2).
Benzimidazole: a medicinally important heterocyclic moiety
Medicinal Chemistry Research
Benzimidazole nucleus is a constituent of many bioactive heterocyclic compounds that are of wide interest because of their diverse biological and clinical applications. Moreover, benzimidazole derivatives are structural isosters of naturally occurring nucleotides, which allows them to interact easily with the biopolymers of the living system. This created interest in researchers who have synthesized variety of benzimidazole derivatives and screened them for their various biological activities, viz., anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimycobacterial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant as well antidiabetic activities.
Benzimidazole: An Important Biological Heterocyclic Scaffold
Journal of Current Pharma Research, 2014
Various heterocyclic scaffolds have drawn special attention of medicinal chemists and hence, extensive efforts are being carried out in search of lead molecules related to it. Benzimidazole is an important pharmacophore owing to its inherent properties and therapeutic actions. These exhibit many biological activities like anticancer, anticonvulsant, antiHIV, antimicrobial and many more. Such biological applications of benzimidazole derivatives have attracted attention and stimulated new search for its novel derivatives with improved biological activities and these are being extensively studied. The present review includes rigorous literature survey on the search of biologically active benzimidazole ring linked and fused with other heteroaromatic systems.
Benzimidazole: A Milestone in the Field of Medicinal Chemistry
Mini-Reviews in Medicinal Chemistry, 2020
In the last 2-3 decades, the broad research in the application of benzimidazole derivatives made it important for mankind. Many scientists have worked on benzimidazole derivatives and they found that this compound has a diverse role in the field of medicinal chemistry. Few benzimidazole derivatives are currently in the market as a drug candidate against various diseases. Moreover, the benzimidazole derivatives exhibit pharmacological activities such as anti-tuberculosis, anti-malarial, antihistamine, antimicrobial, antiviral, antidiabetic, anticancer, anti-fungal, anti-inflammatory, analgesic, anti-HIV, etc. In this review, we have summarized various derivatives of benzimidazole which have been prepared by many researchers to understand the chemistry as well as diverse pharmacological activities. These findings may lead the scientists who are working in the field of medicinal chemistry to the development of benzimidazole based drug candidates in the future.
BMC Chemistry
Background: Nitrogen containing heterocycles are widely used and investigated by pharmaceutical industry, as they are important in discovery and designing of new drug molecules. Drugs with a benzimidazole nucleus possess exclusive structural features and electron-rich atmosphere, which enable them to bind to a number of biologically important targets and result in a wide range of activities. This has served as the basis of the present study whereby new scaffolds with benzimidazole moiety were designed and synthesized. Methods: The structures of synthesized compounds were confirmed by physicochemical and spectral means. The synthesized compounds were screened for their antimicrobial and antiproliferative activities by tube dilution and Sulforhodamine B (SRB) assays, respectively. Results and conclusion: The in vitro biological screening results revealed that compound Z24 exhibited promising antimicrobial and anticancer activities which are comparable to standards.
Synthesis and antimicrobial studies of some novel benzimidazole derivatives
A series of 2-substituted phenoxymethyl benzimidazoles and 1-alkyl-2-substituted phenoxymethyl benzimidazoles (R1X 1-4 -R8X 1-4 ) were prepared. The structures of the benzimidazole derivatives were confirmed on the basis of spectral data. The compounds were screened for their in vitro antibacterial, antifungal, antituberculars activity using bacterial strains (E. Coli, Pseudomonas aeruginosa and Coagulase positive Staphylococcus aureus {COPS}), fungal strains (Candida albicans and Aspergillus niger) and Mycobacterium tuberculosis H 37 RV strain. The results of preliminary screening showed that all synthesized 2-(substituted phenoxymethyl) 1-H benzimidazoles and 1alkyl-2-(substituted phenoxymethyl) benzimidazoles has potential antifungal activity against Candida Albicans, but only few compounds showing activity against Aspergillus niger. Similarly all molecules showed good antibacterial activity against E.coli and Pseudomonas aeruginosa, but very few were resistance to Staphylococcus aureus. And all the synthesized compounds showed good activity against Mycobacterium tuberculosis even at 1 mcg/ml concentration.
IJC-B Vol.60B(01) [January 2021], 2021
Benzimidazole is the heterocyclic compound formed by the fusion of benzene and imidazole ring. Benzimidazole analogs are of great significance because of their clinical application and biological activity. Benzimidazoles are considered as an optimistic class of bioactive heterocyclic compound that possesses a range of biological activities. We have synthesized five substituted Benzimidazole derivative using on both microwave irradiation and conventional heating method. The newly synthesized compounds are characterized by IR, NMR and Mass spectra analysis. In the present study, we have reported the synthesis, spectral studies and biological evaluation of some benzimidazole derivatives. Benzimidazole play important role in medical field with so many pharmacological activities such as antimicrobial, anti bacterial, etc. The potency of this clinically useful drug in treatment in microbial action and other activities has encouraged the development of some more potent and significant compounds.
Benzimidazole: A short review of their antimicrobial activities
International Current Pharmaceutical Journal, 2012
Benzimidazole is the heterocyclic compound formed from benzene and imidazole ring containing nitrogen, oxygen sulphor and its derivatives are of wide interest because of their diverse biological activity and clinical applications, they are remarkably effective compounds both with respect to their inhibitory activity and their favourable selectivity ratio. Reported nucleus is a constituent of vitamin-B12. Benzimidazoles are regarded as a promising class of bioactive heterocyclic compounds that exhibit a range of biological activities like anti-microbial, anti-viral, anti-diabetic, anticancer activity, numerous anti-oxidant, anti-parasitic, anti-helmintics, anti-proliferative, anti-HIV, anti-convulsant, anti-inflammatory, anti-hypertensive, anti-neoplastic, proton pump inhibitor and anti-trichinellosis. Benzimidazoles exhibit significant activity as potential antitumor agents, smooth muscle cell proliferation inhibitors, a treatment for intestinal cystitis, and in diverse area of chemistry. Some of the important benzimidazole derivatives have been reported as thyroid receptor agonist gonadotropin releasing hormone receptor antagonists, non-nucleoside HIV-1 reverse transcriptase inhibitors and interestingly alkynylbenzimidazoles as modulators of metabotropic glutamate receptors. The imidazole core is a common moiety in a large number of natural products and pharmacologically active compounds. The synthesis of novel benzimidazole derivatives remains a main focus of medicinal research. This comprehensive overview summarizes the chemistry of different derivative of substituted benzimidazole along with their anti-microbial activity containing anti-malarial anti-fungal, anti-bacterial, anti-viral activities.