204514-10-3Relevant academic research and scientific papers
Synthesis and antimicrobial activity of some novel 2-[4-(substituted piperazin-/piperidin-1-ylcarbonyl)phenyl]- 1 H-benzimidazole derivatives
Kus, Canan,Soezuedoenmez, Fatma,Altanlar, Nurten
experimental part, p. 54 - 60 (2009/06/18)
In this study, we report the synthesis and antimicrobial evaluation of several new 4-(1H-benzimi-dazol-2-yl)benzamides (11 - 30) and 5-chloro-1-(p-fluorobenzyl)-2-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl} -1H-benzimidazole (33). Compound 20 exhibited the best antibacterial activity with MIC value of 6.25 μg/mL against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA). Significant antifungal activities were obtained with the compounds 13, 14, 18, 19, and 33 with MIC values of 3.12 μg/mL which are close to fluconazole.
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
Zhang, Rui,Lei, Lin,Xu, Yun-Gen,Hua, Wei-Yi,Gong, Guo-Qing
, p. 2430 - 2433 (2008/04/18)
A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.
Substituted 2-phenyl-benzimidazole derivatives: novel compounds that suppress key markers of allergy
Richards, Mark L.,Lio, Shirley Cruz,Sinha, Anjana,Banie, Homayon,Thomas, Richard J.,Major, Michael,Tanji, Mark,Sircar, Jagadish C.
, p. 950 - 969 (2007/10/03)
The pharmacotherapy of allergy and asthma has traditionally focused on the effecter molecules of the allergic cascade, while neglecting targets that play an early role in their development. Reasoning that IgE is central to the expansion of atopic diseases, we identified and extended a novel family of 2-(substituted phenyl)-benzimidazole inhibitors of IgE response. Pharmacological activity depends on an intact phenylbenzimidazole-bis-amide backbone, and is optimized by the presence of lipophilic terminal groups composed of either bis cycloalkyl or combinations of aliphatic and halogen-substituted aromatic groups. These compounds also inhibit IL-4 and IL-5 responses in T cells and CD23 expression on B cells, with potencies that parallel their inhibition of IgE. The broad profile of these compounds thus underscores their potential for treating the multifarious pathology of asthma.
Novel anti-inflammatory and analgesic heterocyclic amidines that inhibit nitrogen oxide (NO) production
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Page/Page column 29, (2010/02/13)
Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which:G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; andZ is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
Novel anti-inflammatory and analgesic heterocyclic amidines that inhibit nitrogen oxide (NO) production
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Page/Page column 20-21, (2010/02/13)
Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
Benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
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, (2008/06/13)
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to benzimidazole molecules tha
Benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
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, (2008/06/13)
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to benzimidazole molecules tha
Single bead IR monitoring of a novel benzimidazole synthesis
Sun, Qun,Yan, Bing
, p. 361 - 364 (2007/10/03)
A novel and efficient solid-phase synthesis of benzimidazoles and the monitoring of all conversions in this synthesis are reported.
