No abstract

The present work is aimed to report several new synthetically and medicinally important pyrazole derivatives. Herein, a series of new 3‐amino‐4‐((3‐aryl‐1‐phenyl‐1H‐pyrazol‐4‐yl) methylene)‐1H‐pyrazol‐5(4H)‐ones (4) were synthesized by the reaction of ethyl 2‐cyano‐3‐(3‐aryl‐1‐phenyl‐1H‐pyrazol‐4‐yl) acrylates (3) and hydrazine hydrate in good yields. All the fourteen compounds (3 and 4) were evaluated for the in vitro antibacterial activity against, Staphylococcus aureus and Bacillus subtilis (Gram Positive), Escherichia coli and Pseudomonas aeruginosa (Gram negative) and the antifungal activity against Candida albicans and Saccharomyces cerevisiae. The tested compounds were found to be active against both the Gram positive strains.

An effective method for the synthesis of 3,3-diaryl-2-(2-oxo-2H-1,4-benzoxazin-3-yl)propanoic acid esters is reported. A novel zinc triflate-catalyzed regioselective 1,6-conjugate addition of vinylogous carbamates to p-quinone methides for accessing the title compounds has been developed. This protocol furnished the hybrid compounds in good to excellent yields. The reaction is rapid and has a broad substrate scope.