Corrigendum to “Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives” [Bioorg. Med. Chem. Lett. 15 (2005) 2265]

Copper(I)-Catalyzed Synthesis of Substituted 2-Mercapto Benzimidazoles

“…2-Mercapto benzimidazoles are an important class of heterocycles that are encountered in a number of natural and non-natural biologically active compounds. For example, medicinal chemistry applications of such compounds include 2-(benzylthio)-4,6-dichloro-1-[(2-hydroxyethoxy)methyl]benzimidazole as an antiviral compound, 2-mercapto-1-(β-4-pyridethyl)benzimidazole (MPB) as an antitumor agent, and luteinizing hormone-releasing hormone (LHRH) antagonists (Figure ) . The cyclic thioureide structure is recognized for its antithyroid action, and has shown atypical antipsychotic potency when linked to aryl piperazines .…”

“…The main methodology for the synthesis of unsymmetrically substituted 2-mercapto benzimidazoles involves the reaction of o -phenylenediamine precursors with CS 2 , followed by alkylation. ,,, Similarly, benzimidazole thiones are prepared from o -phenylenediamine via the formation of benzimidazolones, and thionation of the later with Lawesson’s reagent . These methods suffer from a limited number of suitable substrates for diverse synthesis.…”

Synthesis of various 1‐alkylbenzimidazole derivatives directly from 2‐alkylaminonitroarenes via a two‐step, one‐pot procedure

“…This seemed worthy of investigation because the literature on the biological activity of benzimidazoles shows that, apart from 1-unsubstituted derivatives, those with an alkyl or aralkyl group on the nitrogen atom are clearly more represented than those substituted with any aryl group [1]. In the particular case of 2-thiobenzimidazole D (Figure 1), a direct comparison of compounds differing in the substituent at N-1 showed a much stronger activity of N-alkyl than N-aryl derivatives [9].…”

One-Pot, Green Approach Synthesis of 2-Aryl Substituted Benzimidazole Derivatives Catalyzed by Water Extract of Papaya Bark Ash

“…It is well documented that benzimidazole and its derivatives extensively possesing wide range of spectrum of biological activities [8]. These compounds showed selective non-peptide LH-RH antagonist [9], lymphocyte specific kinase inhibitor [10], N-methyl-D-asparatate kinase inhibitor [11], N-methyl-D-aspartate antagonist [12], 5-lipoxygenase inhibitor [13], neuropeptide N-S5B polymerase inhibitor, neuropeptide YY1 receptor antagonist [14], thrombin inhibitors [15] and poly (ADP-ribose) polymerase inhibitors [16], DNA-miner groovebinding agents possess antitumour activity [17], topoisomerase inhibitors, angiotensin II inhibitors and proloferartion inhibitors [18]. In addition, various promising therapeutic applications of benzimidazole of derivatives found in antimicrobial [19], anticancer [20], antiulcer, antifungal [21], antihypertensive [22], herbicides [23], antihistamine activity [24] and other veterinary applications [25].…”