The methods of chemical structural alteration of small organic molecules by using microbes
(fungi, bacteria, yeast, etc.) are gaining tremendous attention to obtain structurally novel and therapeutically
potential leads. The regiospecific mild environmental friendly reaction conditions with the ability
of novel chemical structural modification in compounds categorize this technique; a distinguished
and unique way to obtain medicinally important drugs and their in vivo mimic metabolites with costeffective
and timely manner. This review article shortly addresses the immense pharmaceutical importance
of microbial transformation methods in drug designing and development as well as the role of
CYP450 enzymes in fungi to obtain in vivo drug metabolites for toxicological studies.
Keywords: Microbial bioconversion, regiospecificity, novel drugs, drug metabolites, pharmaceutical leads, CYP450 enzymes.
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