Design, synthesis and docking studies of novel spiroazetidinone substituted steroidal derivatives possessing potent diversified pharmacological properties

Shams Uzzaman, Khan A. A. Abdul Baqi, Mohd Asif, Abad Ali, Hena Khanam, Ashraf Mashrai, Anis Ahmad, Asad U Khan


Steroidal spiroazetidinone derivatives (3, 10-12) were obtained by the multi-step reactions of ketosteroids. It involved Staudinger ketene-imine [2+2] cycloaddition reaction of steroidal iminophenylcholest-5-enes (2, 7-9). The structural assignment of the products was confirmed on the basis of IR, 1H NMR, 13C NMR, MS and analytical data. The synthesized compounds were screened for in vitro antimicrobial activity against different bacterial and fungal strains by agar diffusion method and in vitro antioxidant activity by using DPPH method. Docking studies were performed to investigate the hypothetical binding mode of the steroidal spiroazetidinones. The results suggest that steroidal bearing a core spiroazetidinone scaffold would be potent phramacological agents.

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