Author
Monika Gaba
Bio: Monika Gaba is an academic researcher from Punjab Technical University. The author has contributed to research in topics: Benzimidazole & Type 2 diabetes. The author has an hindex of 8, co-authored 10 publications receiving 538 citations.
Papers
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TL;DR: In the present review, published reports on benzimidazole scaffold are collated to provide an insight so that its full therapeutic potential can be utilized for the treatment of pain and inflammation.
236 citations
TL;DR: This review enlightens the landscape of the discovery and development of imidazoles- and benzimidazole-based drugs with an emphasis on structure activity relationship features (SAR), medicinal chemistry, and their mechanism of action.
Abstract: Imidazole and benzimidazole rings are the most important nitrogen-containing heterocycles, which are widely explored and utilized by the pharmaceutical industry for drug discovery. Due to their special structural features and electron-rich environment, imidazole- and benzimidazole-containing drugs bind to a variety of therapeutic targets, thereby exhibiting a broad spectrum of bioactivities. Numerous imidazole- and benzimidazole-based drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potential. Due to their enormous medicinal value, the research and development of imidazole- and benzimidazole-containing drugs is an increasingly active and attractive topic of medicinal chemistry. This review enlightens the landscape of the discovery and development of imidazole- and benzimidazole-based drugs with an emphasis on structure activity relationship features (SAR), medicinal chemistry, and their mechanism of action. Furthermore, the present review also provides the recent advances in the development of imidazole- and benzimidazole-based drugs along with new perspectives. We hope that this paper will open up new opportunities for researchers to design future generation novel and potent imidazole- and benzimidazole-containing drugs.
196 citations
TL;DR: A series of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives exhibited moderate to good anti-inflammatory and analgesic activity in carrageenan-induced rat paw edema and acetic acid-induced writhing in mice, respectively, with low ulcerogenicity compared with the standard drug indomethacin.
97 citations
TL;DR: In this paper, the synthesis and biological evaluation of N-1-(phenylsulfonyl)-2-methylamino-substituted-1H-benzimidazole derivatives with lower GI toxicity was described.
53 citations
TL;DR: A series of 1-methyl-N-((substituted-phenylmethylidene)-1H-benzimidazol-2-amines (4a-4g) were prepared via the formation of 1methyl-1-h-benzmanidazolate-2.2-amine (3), which was pre- pared by the cycloaddition of ophenylenediamine (1) with cyanogen bromide in the presence of aqueous base followed by N-methylation with methyl iodide in
39 citations
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TL;DR: This review reports on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals, and reports detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.
Abstract: Nitrogen heterocycles are among the most significant structural components of pharmaceuticals. Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule drugs contain a nitrogen heterocycle. In this review we report on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of our analysis is divided into seven sections: (1) three- and four-membered heterocycles, (2) five-, (3) six-, and (4) seven- and eight-membered heterocycles, as well as (5) fused, (6) bridged bicyclic, and (7) macrocyclic nitrogen heterocycles. Each section reveals the top nitrogen heterocyclic structures and their relative impact for that ring type. For the most commonly used nitrogen heterocycles, we report detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.
3,241 citations
TL;DR: In the present review, various derivatives of benzimidazole with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for developing an SAR on benzimdazole derived compounds for each activity.
584 citations
TL;DR: It is shown that imidazole propionate is produced from histidine in a gut simulator at higher concentrations when using fecal microbiota from subjects with versus without type 2 diabetes and that it impairs glucose tolerance when administered to mice.
439 citations
TL;DR: The benefit of the incorporation of mucoadhesive polymers into the structure of these innovative pharmaceutical products to prolong their residence time in the administration site and the release of the drug cargo will be discussed with focus in the developments of the last decade.
388 citations
TL;DR: In the present review, published reports on benzimidazole scaffold are collated to provide an insight so that its full therapeutic potential can be utilized for the treatment of pain and inflammation.
236 citations