Microwave Assisted and Al2O3/K2CO3 Catalyzed Synthesis of Azetidin-2-One Derivatives Containing Aryl Sulfonate Moiety with Anti-Inflammatory and Anti-Microbial Activity

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 anti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs. Antimicrobial activity of all synthesized compounds has been tested and most of the compounds showed good anti-bacterial and anti-fungal activities.

Antimicrobial and Anti-Inflammatory Activity Studies of Novel Thiazolopyrimidines

“…In view of the above and in continuation of our previous work in heterocyclic chemistry [23] herein we submit a report of our findings on the synthesis and pharmacological evaluation of new thiazolopyrimidines.…”

Untitled

“…[1][2][3][4][5][6] In the present study, Isoniazid (INH), the established antitubercular drug was selected as the lead for the design and development of antitubercular agents with minimal toxic effects. A novel series of amino azetidinones were designed from corresponding azetidin-2-ones using various in silico methods.…”