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Background  Aminoquinoline/steroid conjugates were synthesized based on the fact that steroid transporters have been shown to accept and carry a variety of drugs. So, in continuing our research of antileishmanial and antitubercular drugs, aminoquinoline/steroid conjugates ( 12 ,  13,  and  14)  were regioselectively synthesized via 1, 3-dipolar cycloaddition of alkynes  3, 5 , and  7  with azide  12 . The aminoquinoline/steroids conjugates were evaluated  in vitro  against  Leishmania major  and  Mycobacterium tuberculosis .    Results  Regioselective synthesis of the novel aminoquinoline/steroid conjugates was achieved in very high yield. All aminoquinoline/steroid conjugates ( 12 ,  13,  and  14 ) exhibited best results against  Leishmania  and  M. tuberculosis  than the respective alkyne intermediate structures ( 3 ,  5,  and  7 , respectively). Among them, the compound  12  exhibited the best activity for  M. tuberculosis  (MIC = 8.8 μM). This result is comparable to drugs commonly used in tuberculosis treatment. Also, for antileishmanial assay, the aminoquinoline/steroid conjugates demonstrated a significant activity against promastigote and amastigote forms of  L. major .    Conclusions  Addition of a steroid group to aminoquinoline molecules enhanced the leishmanicidal and antitubercular activities. These results highlight the importance of steroids as carrier.

Increase of leishmanicidal and tubercular activities using steroids linked to aminoquinoline