Benzimidazole: An emerging scaffold for analgesic and anti-inflammatory agents

Gaba, Monika; Singh, Sudhakar; Mohan, Chander

doi:10.1016/j.ejmech.2014.01.030

Cited by 281 publications

(136 citation statements)

References 60 publications

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“…Omeprazole 3 and Pimobendan 4 that are therapeutically useful in the management of peptic ulcer and congestive heart failure, respectively. Many derivatives of benzimidazoles are well known for their antimicrobial, [5][6][7][8][9][10] anthelmintic, 11 antiviral, [12][13][14][15][16] and antifungal 17,18 activities. Since 1985 benzimidazole containing compounds have been reported as well known anticancer agents.…”

Section: Introductionmentioning

confidence: 99%

New approaches for the synthesis, cytotoxicity and toxicity of heterocyclic compounds derived from 2-cyanomethyl benzo[c]imidazole

Mohareb

Mohamed²,

Abdallah³

2016

ACSi

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The reaction of ethyl cyanoacetate with o-phenylenediamine gave the 2-cyanomethylbenzo[c]imidazole (1). The latter compound was used as the key starting material to synthesise biologically active heterocyclic derivatives. Thus, the reaction of 1 with cyclohexanone and either of benzaldehyde, 4-methoxybenzaldehyde or 4-chlorobenzaldehyde gave the annulated derivatives 2a-c, respectively. The antitumor evaluations of the newly synthesized products against the three cancer cell lines MCF-7 (breast adeno-carcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) showed that compounds 2b, 6, 11b, 11c, 12b, 16a, 16b and 18a exhibited optimal cytotoxic effect against cancer cell lines, with IC 50 values in the nM range. Bioactive compounds are often toxic to shrimp larvae. Thus, in order to monitor these chemicals in vivo lethality to shrimp larvae (Artemia salina), Brine-Shrimp Lethality Assay was used. Compounds 11b, 12b and 16b showed no toxicity against the tested organisms.

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Section: Introductionmentioning

confidence: 99%

New approaches for the synthesis, cytotoxicity and toxicity of heterocyclic compounds derived from 2-cyanomethyl benzo[c]imidazole

Mohareb

Mohamed²,

Abdallah³

2016

ACSi

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“…Azole class of drugs, particularly fused imidazole occupy prominent place in medicinal chemistry because of their broad spectrum of pharmacological activities such as anti-inflammatory, analgesic, anticancer, antiulcer, antimicrobial, antiviral, pesticidal, cytotoxicity, and anti-arrhythmic activities [2][3][4][5]. Omeprazole, Mebendazole, and Albendazole are well known drugs in the market which contain fused imidazole as active core moiety.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2015

BAOJPS

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“…Retaining fluorine in a molecule is also desirable from a medicinal chemistry perspective, since fluorine can improve resistance to metabolism due to the strong C-F bond (485 kJmol -1 ) while the small size (van der Waals radius, 1.47 Å) and high electronegativity (3.98 Pauling scale) endow specific electronic properties that can dramatically alter the biological response of the compound [14,15]. Benzimidazoles, amongst other aza-heterocycles, represent privileged substructures in medicinal chemistry and serve as desirable building blocks in the design and construction of bioactive compounds [16,17,18]. Here we report the synthesis of a number of N-fluoroaryl benzimidazole derivatives using S N Ar substitution of perfluorinated arenes and the screening of these for activity against breast carcinoma MCF-7, leukemia K562, melanoma G361 and osteosarcoma HOS cell lines.…”

Section: Introductionmentioning

confidence: 99%