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  • Title: Solid-phase synthesis of a library of pyrrolo[2,1-c][1,4]benzodiazepine-5,11-diones with potential antitubercular activity.
    Author: Kamal A, Reddy KL, Devaiah V, Shankaraiah N, Reddy GS, Raghavan S.
    Journal: J Comb Chem; 2007; 9(1):29-42. PubMed ID: 17206830.
    Abstract:
    A versatile combinatorial approach was developed and utilized for the rapid synthesis of pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dione (PBD-5,11-dione) libraries 10, 15, and 19 containing 210 compounds with varied substitutions in A, B, and C rings. The key aspect of the synthetic strategy includes Staudinger, intermolecular aza-Wittig reaction followed by imine reduction and base-mediated cyclative cleavage results in the formation of final resin-free compounds. This strategy provides a highly efficient and practical protocol for the parallel synthesis of PBD-5,11-diones on solid support. The modifications in the C-ring of the PBD scaffold produced three types of sublibraries. Reactions were monitored by FT-IR spectroscopy on the resin beads. Further, from a generated library of 210 compounds, 142 compounds have been selected and evaluated for in vitro activity against Mycobacterium tuberculosis, and some of these compounds have exhibited promising activity.
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