Computer assisted designing (CADD), insilico pharmacological studies followed by synthesis and characterization of garcinosporin a novel semisynthetic β-lactam antibiotic

The drug discovery and designing team is always being keen to find out newer and newer remedies for the industry but they have to cross many hurdles as the development of new drugs with potential therapeutic applications is one of the most complex and difficult process in the pharmaceutical industry. The emergence of superbugs and antibiotic resistance due to the incorrect usage and dosage of antibiotics is one of the serious threats in front of the team for many reasons. One of the solutions that can be adopted to overcome this hurdle is the designing of the new drug based on the natural product of proven therapeutic value and other one is the suitable derivatization of the existing drugs. The present research also looking to the world of natural products to make a new antibiotic based on both traditional and modern knowledge. The starting materials selected were Garcinia acid (Hydroxy citric acid) an active ingredient of many Ayurvedic drugs and 7-ACA the core part of Cephalosporins. The selected lead was modified and designed with simple application of computer assisted drug designing (CADD) and insilico pharmacological and toxicological studies to understand the druggability of the lead selected. This was followed by actual synthesis and characterization using spectroscopic methods. The resulted novel antibiotic is named as Garcinosporin belong to the class of semisynthetic β-lactam cephalosporin type

Author(s): Abhilash Mullasseril

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