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Background  Biotransformation is an effective technique for the synthesis of libraries of bioactive compounds. Current study on microbial transformation of dihydrotestosterone (DHT) ( 1 ) was carried out to produce various functionalized metabolites.    Results  Microbial transformation of DHT ( 1 ) by using two fungal cultures resulted in potent butyrylcholinesterase (BChE) inhibitors. Biotransformation with  Macrophomina phaseolina  led to the formation of two known products, 5α-androstan-3β,17β-diol ( 2 ), and 5β-androstan-3α,17β-diol ( 3 ), while biotransformation with  Gibberella fujikuroi  yielded six known metabolites, 11α,17β-dihydroxyandrost-4-en-3-one ( 4 ), androst-1,4-dien-3,17-dione ( 5 ), 11α-hydroxyandrost-4-en-3,17-dione ( 6 ), 11α-hydroxyandrost-1,4-dien-3,17-dione ( 7 ), 12β-hydroxyandrost-1,4-dien-3,17-dione ( 8 ), and 16α-hydroxyandrost-1,4-dien-3,17-dione ( 9 ). Metabolites  2  and  3  were found to be inactive, while metabolite  4  only weakly inhibited the enzyme. Metabolites  5 – 7  were identified as significant inhibitors of BChE. Furthermore, predicted results from docking simulation studies were in complete agreement with experimental data. Theoretical results were found to be helpful in explaining the possible mode of action of these newly discovered potent BChE inhibitors. Compounds  8  and  9  were not evaluated for enzyme inhibition activity both  in vitro  and  in silico , due to lack of sufficient quantities .Conclusion  Biotransformation of DHT ( 1 ) with two fungal cultures produced eight known metabolites. Metabolites  5 – 7  effectively inhibited the BChE activity. Cholinesterase inhibition is among the key strategies in the management of Alzheimer’s disease (AD). The experimental findings were further validated by  in silico  inhibition studies and possible modes of action were deduced.

Molecular docking simulation studies on potent butyrylcholinesterase inhibitors obtained from microbial transformation of dihydrotestosterone