Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.

The efficient and rapid synthesis of 5-nitro-2-aryl substituted-1H-benzimidazole libraries (1a-1j) has been established. Thus, both microwave and conventional cyclo-condensation of 4-nitro ortho-phenylenediamine with various phenoxyacetic acids were carried out in the presence of HCl catalyst. The m...

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Main Authors: Hosamani, K, Seetharamareddy, H, Keri, R, Hanamanthagouda, MS, Moloney, M
Formato: Journal article
Idioma:English
Publicado em: 2009
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author Hosamani, K
Seetharamareddy, H
Keri, R
Hanamanthagouda, MS
Moloney, M
author_facet Hosamani, K
Seetharamareddy, H
Keri, R
Hanamanthagouda, MS
Moloney, M
author_sort Hosamani, K
collection OXFORD
description The efficient and rapid synthesis of 5-nitro-2-aryl substituted-1H-benzimidazole libraries (1a-1j) has been established. Thus, both microwave and conventional cyclo-condensation of 4-nitro ortho-phenylenediamine with various phenoxyacetic acids were carried out in the presence of HCl catalyst. The microwave synthesis route afforded advantages, such as good to excellent yields, shorter reaction time (2.5-3.5 min), readily available starting material, and simple purification procedure, which distinguish the present protocol from other existing methods used for the synthesis of benzimidazole libraries. Bioassay indicated that all the compounds showed in vitro antimicrobial activity against Vancomycin resistant enteroccoccus, Staphylococcus aureus, Micrococcus, Bacillus subtilis (gram-positive bacteria) and Shigella dysentery, Escherichia coli (gram-negative bacteria) and Candida albicans, Aspergillus niger, Penicillium (fungi). The minimum inhibitory concentration (MIC) was determined for test compounds as well as for reference standards.
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spelling oxford-uuid:dc926a4f-0fc2-4676-a287-cd324bae4e832022-03-27T09:18:40ZMicrowave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:dc926a4f-0fc2-4676-a287-cd324bae4e83EnglishSymplectic Elements at Oxford2009Hosamani, KSeetharamareddy, HKeri, RHanamanthagouda, MSMoloney, MThe efficient and rapid synthesis of 5-nitro-2-aryl substituted-1H-benzimidazole libraries (1a-1j) has been established. Thus, both microwave and conventional cyclo-condensation of 4-nitro ortho-phenylenediamine with various phenoxyacetic acids were carried out in the presence of HCl catalyst. The microwave synthesis route afforded advantages, such as good to excellent yields, shorter reaction time (2.5-3.5 min), readily available starting material, and simple purification procedure, which distinguish the present protocol from other existing methods used for the synthesis of benzimidazole libraries. Bioassay indicated that all the compounds showed in vitro antimicrobial activity against Vancomycin resistant enteroccoccus, Staphylococcus aureus, Micrococcus, Bacillus subtilis (gram-positive bacteria) and Shigella dysentery, Escherichia coli (gram-negative bacteria) and Candida albicans, Aspergillus niger, Penicillium (fungi). The minimum inhibitory concentration (MIC) was determined for test compounds as well as for reference standards.
spellingShingle Hosamani, K
Seetharamareddy, H
Keri, R
Hanamanthagouda, MS
Moloney, M
Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.
title Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.
title_full Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.
title_fullStr Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.
title_full_unstemmed Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.
title_short Microwave assisted, one-pot synthesis of 5-nitro- 2-aryl substituted-1H-benzimidazole libraries: screening in vitro for antimicrobial activity.
title_sort microwave assisted one pot synthesis of 5 nitro 2 aryl substituted 1h benzimidazole libraries screening in vitro for antimicrobial activity
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