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Sriram, D. et al.

Sriram, Yogeeswari, Gopal,

Synthesis, anti-HIV and antitubercular activities of lamivudine prodrugs.

The synthesis of a novel series of lamivudine prodrugs involving N4-substitution with isatin derivatives is described. The in-vitro antiretroviral activities indicated that compound 3b was found to be equipotent to lamivudine with EC50 of 0.0742+/-0.04 microM. Lamivudine prodrugs bearing fluoroquinoles antibacterial showed 92-100% inhibition against Mycobacterium tuberculosis strain H37Rv at 6.25 microg ml(-1). At pH 7.4, 37 degrees C, the hydrolytic t(1/2) ranged between 120 and 240 min.[1]

References

Synthesis, anti-HIV and antitubercular activities of lamivudine prodrugs. Sriram, D., Yogeeswari, P., Gopal, G. European journal of medicinal chemistry. (2005) [Pubmed]

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