Abstract
We report the novel synthesis of azetidin-2-one derivatives containing aryl sulfonate moiety from the reaction of 2-hydroxy benzaldehyde with p-toluene sulfonyl chloride afforded firstly 2-formylphenyl 4-methylbenzene sulfonate (2). The compound (2) on reaction with p-aminobenzoic acid or 2-aminopyridine gave the corresponding aldimines (3). Furthermore, the aldimines are on reaction with chloroacetyl chloride gives corresponding azetidin-2-ones in good to moderate yield. Among the eight synthesized azetidin-2-ones, five selected compounds have been screened for the an-ti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs. Anti- microbial activity of all synthesized compounds has been tested and most of the compounds showed good anti-bacterial and anti-fungal activities.
Highlights
The synthesis of new compounds and their biological screening is recently of enormous focus within the synthetic and medicinal chemistry communities
We report the novel synthesis of azetidin-2-one derivatives containing aryl sulfonate moiety from the reaction of 2-hydroxy benzaldehyde with p-toluene sulfonyl chloride afforded firstly 2-formylphenyl 4-methylbenzene sulfonate (2)
Among the eight synthesized azetidin-2-ones, five selected compounds have been screened for the anti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs
Summary
The synthesis of new compounds and their biological screening is recently of enormous focus within the synthetic and medicinal chemistry communities. Azetidin2-ones are well known antibiotics containing β-lactam monocyclic ring and reported to exhibit interesting biological activities. They are mostly prescribed medicines to treat bacterial infections. They were found to possess powerful anti-microbial [1,2], anti-proliferative [3], IFN-gamma [4], cytotoxic [5], anticonvulsant, anti-tubercular [6], cholesterol absorption inhibitor [7], antiinflammatory and anti-degenerative activities [8]. It was envisaged that the compounds containing both the chemical moieties would result in new compounds of interesting biological activities. Five selected compounds of this library were screened for the anti-inflammatory activity. All compounds synthesized in this series have been screened for anti-bacterial and anti-fungal activities
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