Biotransformation is a process by which organic compounds are transformed from one form to another, aided by organisms such as bacteria, fungi and enzymes. Biotransformations are used as a valuable strategy to build molecules, similar to parent drug in the drug discovery programme. Biotransformations can also be used to synthesize compounds or materials, if synthetic approaches are challenging. Microbial biotransformations or microbial biotechnology are extensively used to generate metabolites in bulk amounts. Biotransformation approaches and synthetic methods in tandem provide a source for generating compounds around core structures, which can be screened for various biological activity studies. These studies help in screening and advancing the compounds, through various stages of drug discovery programme. Hence, biotransformation experiments can be effectively utilized to synthesize more compounds.