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Biotransformation is a process by which organic compounds are converted from one form to another with the aid of organisms
such as enzymes, bacteria and fungi. In the drug discovery programme biotransformations are used as a valuable strategy
to build molecules similar to parent drug. Biotransformations can also be used to synthesize molecules which are difficult by
synthetic approaches. Microbial biotransformations are widely used to generate metabolites in gram quantities. Biotransformation
and synthetic approaches in tandem serves as a vital source for generating compounds around core structures which can be
screened for various activity studies to advance the compounds. During pre-clinical stage, information from biotransformation
experiments can be effectively utilized to synthesize more back-up compounds.
Sulfonylurea urea drugs were incubated with hepatic microsomes to produce metabolites. For example one of the sulfonylurea
urea drugs in the market shows new metabolites which are characterized using liquid chromatography and mass spectrometry.
Liquid chromatography is used to separate the formed metabolites. Fragmentation pattern from the mass spectrum is utilized to
identify the biotransformation site in the molecule which is the metabolic soft spot. Neutral loss scan in the mass spectrometer is
used to identify adducts of the drugs. Identified new metabolites are structurally similar to parent drugs implying the possibility
of better therapeutic effects. Formed new metabolites are due to the activity of different type of enzymes in hepatic microsomes.
Selvan Ravindran is a Senior Research Scientist in Sai Life Sciences Limited, Pune, India. He received his Ph.D degree from Indian Institute
of Technology (Chennai). He did his postdoctoral studies in University of Texas Medical Branch, USA and University of Arizona, USA. He also
worked as a Biotransformation Scientist in Biocon Bristol Myers and Squibb Research Centre in Bangalore. His major areas of research interests
are Biotransformation (Metabolite identification using liquid chromatography and mass spectrometry), Bioanalysis and DMPK (Drug Metabolism
and Pharmacokinetics). He has published more than 10 research papers in reputed journals and presented more than 15 papers in national and
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