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Current Organic Synthesis

Author(s): Sultanat*, Anam Ansari, Mohd Qamar, Shafiullah, Sartaj Tabassum and Firoz A. Ansari

DOI: 10.2174/1570179417666201218164112

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Multi-Component One-Pot Assisted Synthesis, Anti-bacterial Capabilities, and Scanning Electron Microscopy of Novel Corticosteroid Thiopyran

Page: [411 - 417] Pages: 7

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Abstract

Background: Corticosteroids are an important group of polycyclic compounds having a wide range of pharmacological and physiological properties. Thiopyran derivatives are important building blocks of many biologically active compounds.

Objective: Keeping in mind the wide range of applications of corticosteroids and thiopyran, herein we intend to develop a simple and efficient strategy to synthesize steroidal thiopyran derivatives starting with different commercially available corticosteroids and study their biological properties.

Materials and Methods: To achieve our aim, we employed a one-pot multi-component synthesis of steroidal thiopyran derivatives by the reaction of corticosteroids, malononitrile, and carbon disulphide in the presence of triethylamine as a catalyst.

Results and Discussion: An array of novel thiopyran compounds was obtained with the highest product yield using Et3N. Scanning electron microscopy analysis manifested agglomeration pertaining to brick-shaped crystals of corticosteroid thiopyran. Synthesized compounds were also found to be active as anti-bacterial agents.

Conclusion: We describe a facile one-pot multi-component synthesis of corticosteroid thiopyran derivatives, which are found to possess anti-bacterial activity. Excellent yields of the products, simple work-up, easily available starting materials, and non-chromatographic purification are some of the main advantages of this protocol.

Keywords: Corticosteroid, thiopyran, anti-bacterial, malononitrile, carbon disulphide, Et3N.

Graphical Abstract

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