Benzimidazole: a medicinally important heterocyclic moiety

Narasimhan, Balasubramanian; Sharma, Deepika; Kumar, Pradeep

doi:10.1007/s00044-010-9533-9

Cited by 203 publications

(93 citation statements)

References 56 publications

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“…The performed biological studies shown that the activity varies between the Compounds bearing, respectively, benzene, nitroaniline, or benzoimidazole aromatic ring. Although a wide variety of benzimidazole derivatives have been previously described for their antifungal activity (Kawasaki et al, 2003;Narasimhan et al, 2010), our results showed that benzoimidazolebased halogenomethyl sulfones are the weaker agents against C. albicans wt SC5314 among the all Compounds tested. While benzene-based Compounds were the strongest inhibitors of fungal strains.…”

Section: Discussionmentioning

confidence: 61%

Comparison of anti-Candida albicans activities of halogenomethylsulfonyl derivatives

2014

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A rapidly growing resistance of Candida spp. requires a search for bioactive compounds with fungicidal or fungistatic activity. In this context a characteristics and comparison of antifungal properties of 19 sulfone derivatives were conducted. MICs of the Compounds were determined using the M27-A3 protocol following CLSI recommendations. The SAP expression was analyzed using RT-PCR; relative quantification was normalized against ACT1 in cells grown in YEPD and on Caco-2. 79 % of sulfone derivatives (15 out of 19) exhibited an activity against Candida albicans in the tested concentrations. While the addition of both chlorine and bromine atoms to halogenomethylsulfonyl groups stimulates sulfone's antifungal activity, a chlorine atom more effectively up-regulates antifungal properties of the tested sulfones. The insertion of a fluorine atom has a binary effect on antifungal properties of the tested sulfones. The fluorine atom enhances anti-Candida properties when introduced to the aromatic ring, while its presence in halogenomethylsulfonyl group generally lowers the Compound's efficiency. The deletion of particular SAP genes resulted in an increased susceptibility of C. albicans toward sulfones indicating the role of this gene family in resistance mechanisms. Furthermore, RT-PCR analysis demonstrated that sulfone derivatives inhibit the SAP2 expression but not that of SAP7.

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Section: Discussionmentioning

confidence: 61%

Comparison of anti-Candida albicans activities of halogenomethylsulfonyl derivatives

2014

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“…The synthesized derivatives(PZ1-3) posess 2,3 dione moiety as common, as it has been reported earlier 2,3-dione moiety in the structure of piperazine was considered as promising candidates as an antihelminthic agent 3,16 . In scheme 2, the targeted compounds were synthesized fusing benzimidazole and piperazine through Mannich reaction.…”

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confidence: 84%

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2016

IJPSR

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“…Over the years of active research, benzimidazole is reported to shown wide range of therapeutic activities [1][2][3][4][5][6][7]. Albendazole, mebendazole, thiabendazole as antihelmintics; omeprazole, lansoprazole, pantoprazole as proton pump inhibitors; astemizole as antihistaminic; enviradine as antiviral; candesarten cilexitil and telmisartan as antihypertensive which contains benzimidazole as active pharmacophore.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activity of Some New Imidazolinone Derivatives Containing Benzimidazole

Mehta¹,

Davadra

Shah

et al. 2014

ILCPA

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In this study some new o-benzimidazol-2'-yl-benzamido-p'-benzamido-2-phenyl-4-substituted phenyl-5-oxo-Imidazolines 3a-3j were synthesized. To synthesized target molecules we used various substituted oxazolone derivatives, synthesized from substituted benzaldehyde with hippuric acid. Substituted oxazolones 2a-2j were reacted with carbohydrazide derivative of benzimidazole 1 in presence of pyridine as base to obtained substituted imidazolinone derivatives. All synthesized compounds were characterized by IR, 1 H NMR, elemental analysis and further supported by mass spectroscopy. All synthesized compounds were screened for their antimicrobial activity against gram positive and gram negative bacteria which showed moderate to good activity. All compounds showing good to moderate active against fungal strain as compare to standard drug.

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Benzimidazole: a medicinally important heterocyclic moiety

Cited by 203 publications

References 56 publications

Comparison of anti-Candida albicans activities of halogenomethylsulfonyl derivatives

Comparison of anti-Candida albicans activities of halogenomethylsulfonyl derivatives

Untitled

Synthesis and Antimicrobial Activity of Some New Imidazolinone Derivatives Containing Benzimidazole

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