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  • Title: Synthesis and antimycobacterial activity of prodrugs of indeno[2,1-c]quinoline derivatives.
    Author: Upadhayaya RS, Shinde PD, Kadam SA, Bawane AN, Sayyed AY, Kardile RA, Gitay PN, Lahore SV, Dixit SS, Földesi A, Chattopadhyaya J.
    Journal: Eur J Med Chem; 2011 Apr; 46(4):1306-24. PubMed ID: 21334792.
    Abstract:
    Recently we have reported anti-TB properties of a new class of conformationally-constrained indeno[2,1-c]quinolines, which are although considerably active (MIC 0.39-0.78 μg/mL) suffered from intense solubility problems. We thought of improving their bioavailability by prodrugs approach. Accordingly esters of the "Lead" indeno[2,1-c]quinolines 1, 15 and 27 derivatives were synthesized and their prodrug nature at the physiological pH were confirmed. Prodrugs were evaluated for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv by MABA assay to show that they have 2- to 4-fold improved anti-TB activities, increased aqueous solubility and superior selectivity index over their respective parent compounds. MIC of these prodrugs was in the range of <0.20-6.0 μg/mL, and in general, no cytotoxicity was observed in VERO cells.
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