Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole
2014
Authors
Vasic, Vesna P.Penjišević, Jelena
Novaković, Irena T.
Šukalović, Vladimir
Andrić, Deana
Kostić-Rajačić, Slađana
Article (Published version)
Metadata
Show full item recordAbstract
A series of eight novel 5-substituted derivatives of benzimidazole was synthesized by condensation of the corresponding diamine with ethyl 4-[4-(2-chlorophenyl)piperazin-1-yl]butanoate in refluxing 4 M hydrochloric acid. In vitro antibacterial activity against ten strains, namely Bacillus subtilis, Clostridium sporogenes, Streptosporangium longisporum, Micrococcus flavus, Sarcina lutea, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris and antifungal activity against two fungal strains, namely Candida albicans and Saccharomyces cerevisiae, were evaluated. Of all the compounds screened for activity, 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-iodo-1H-benzimidazole and 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-methyl-1H-benzimidazole were associated with higher antifungal activity than commercial drugs.
Keywords:
arylpiperazines / benzimidazoles / antibacterial activity / antifungal activitySource:
Journal of the Serbian Chemical Society, 2014, 79, 3, 277-282Publisher:
- Serbian Chemical Soc, Belgrade
Funding / projects:
- Structure-activity relationship of newly synthesized biological active compound (RS-MESTD-Basic Research (BR or ON)-172032)
DOI: 10.2298/JSC130418058V
ISSN: 0352-5139
WoS: 000333770600001
Scopus: 2-s2.0-84896935228
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Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Vasic, Vesna P. AU - Penjišević, Jelena AU - Novaković, Irena T. AU - Šukalović, Vladimir AU - Andrić, Deana AU - Kostić-Rajačić, Slađana PY - 2014 UR - https://cherry.chem.bg.ac.rs/handle/123456789/1522 AB - A series of eight novel 5-substituted derivatives of benzimidazole was synthesized by condensation of the corresponding diamine with ethyl 4-[4-(2-chlorophenyl)piperazin-1-yl]butanoate in refluxing 4 M hydrochloric acid. In vitro antibacterial activity against ten strains, namely Bacillus subtilis, Clostridium sporogenes, Streptosporangium longisporum, Micrococcus flavus, Sarcina lutea, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris and antifungal activity against two fungal strains, namely Candida albicans and Saccharomyces cerevisiae, were evaluated. Of all the compounds screened for activity, 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-iodo-1H-benzimidazole and 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-methyl-1H-benzimidazole were associated with higher antifungal activity than commercial drugs. PB - Serbian Chemical Soc, Belgrade T2 - Journal of the Serbian Chemical Society T1 - Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole VL - 79 IS - 3 SP - 277 EP - 282 DO - 10.2298/JSC130418058V ER -
@article{ author = "Vasic, Vesna P. and Penjišević, Jelena and Novaković, Irena T. and Šukalović, Vladimir and Andrić, Deana and Kostić-Rajačić, Slađana", year = "2014", abstract = "A series of eight novel 5-substituted derivatives of benzimidazole was synthesized by condensation of the corresponding diamine with ethyl 4-[4-(2-chlorophenyl)piperazin-1-yl]butanoate in refluxing 4 M hydrochloric acid. In vitro antibacterial activity against ten strains, namely Bacillus subtilis, Clostridium sporogenes, Streptosporangium longisporum, Micrococcus flavus, Sarcina lutea, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris and antifungal activity against two fungal strains, namely Candida albicans and Saccharomyces cerevisiae, were evaluated. Of all the compounds screened for activity, 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-iodo-1H-benzimidazole and 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-methyl-1H-benzimidazole were associated with higher antifungal activity than commercial drugs.", publisher = "Serbian Chemical Soc, Belgrade", journal = "Journal of the Serbian Chemical Society", title = "Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole", volume = "79", number = "3", pages = "277-282", doi = "10.2298/JSC130418058V" }
Vasic, V. P., Penjišević, J., Novaković, I. T., Šukalović, V., Andrić, D.,& Kostić-Rajačić, S.. (2014). Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole. in Journal of the Serbian Chemical Society Serbian Chemical Soc, Belgrade., 79(3), 277-282. https://doi.org/10.2298/JSC130418058V
Vasic VP, Penjišević J, Novaković IT, Šukalović V, Andrić D, Kostić-Rajačić S. Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole. in Journal of the Serbian Chemical Society. 2014;79(3):277-282. doi:10.2298/JSC130418058V .
Vasic, Vesna P., Penjišević, Jelena, Novaković, Irena T., Šukalović, Vladimir, Andrić, Deana, Kostić-Rajačić, Slađana, "Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole" in Journal of the Serbian Chemical Society, 79, no. 3 (2014):277-282, https://doi.org/10.2298/JSC130418058V . .