Abstract
Synthesis of a series of novel and functionalized benzimidazole derivatives by the condensation of OPDA with 4-bromobenzoic acid and subsequent reactions of the product obtained with phenylacetylene and 6-ethynyl-4,4-dimethylthiochroman utilising Sonogashira coupling has been reported. The Sonogashira coupling products were then alkylated at the benzimidazole -NH with different electrophilic reagents leading to functionalized derivatives. All the compounds synthesized were screened for their potential anti-bacterial, anti-asthmatic and anti-diabetic properties, which exhibited moderate activities in screening studies in vitro.
MeSH terms
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Alkynes / chemical synthesis*
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Alkynes / chemistry
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Alkynes / pharmacology
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Anti-Asthmatic Agents / chemical synthesis*
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Anti-Asthmatic Agents / chemistry
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Anti-Asthmatic Agents / pharmacology
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology
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Dipeptidyl-Peptidase IV Inhibitors
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Heterocyclic Compounds, 2-Ring / chemical synthesis*
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Heterocyclic Compounds, 2-Ring / chemistry
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Heterocyclic Compounds, 2-Ring / pharmacology
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Humans
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / chemistry
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Hypoglycemic Agents / pharmacology
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Phosphodiesterase 4 Inhibitors
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Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Alkynes
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Anti-Asthmatic Agents
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Anti-Bacterial Agents
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Benzimidazoles
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Dipeptidyl-Peptidase IV Inhibitors
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Heterocyclic Compounds, 2-Ring
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Hypoglycemic Agents
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Phosphodiesterase 4 Inhibitors
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Protein Tyrosine Phosphatase, Non-Receptor Type 1