Abstract

AbstractAn efficient ferric citrate catalyzed Biginelli reaction is reported to synthesize novel dihydropyrimidin‐(1H)‐ones with free amino group. Diversifying this free amino element provides an access to new and interesting DHMPs for pharmacological profiling. A series of novel dihydropyrimidin‐(1H)‐ones–sulphonamide conjugates were synthesized and evaluated against a panel of Gram positive as well as Gram negative bacteria and fungi. Among the series, the DHMP conjugate 6 a with a 2‐napthyl sulphonamide moiety exhibited excellent antibacterial activity with potency at least four times higher than the standard drugs such as ciprofloxacin, ampicillin and chloramphenicol against the tested bacterial strains.

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