Abstract
Following our previous studies, to affiliate selective pharmacophore in a single molecular entity, domino, ecologically benign, four hetero-component, single pot reaction has been carried out in (bmim)BF4 ionic liquid to structure a new class of compact heteronuclei. In a newly constructed heterocyclic Ugi adducts, quinoline was used as nitrogen source and benzothiazole as well as thiophene moieties were selected to introduce sulphur functionality. This Ugi eco-compatible heterocyclic synthesis resulted in relatively good yields with prompt reaction time. New products were screened for their in vitro antimicrobial activity against a representative panel of bacteria and fungi and some of the final analogues displayed more or equal potency at MIC range 6.25-25 µg/mL than control drugs ampicillin, gentamicin and fluconazole (MICs: 6.25-25 µg/mL). The structural assignments of the new products were done on the basis of FT-IR, 1H NMR spectroscopy and elemental analysis.
Keywords: Thiophehe, Furan, Quinoline, Coumarin, Benzothiazole, Ugi reaction, Antimicrobial activity.
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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