Potential Antimalarial Drug Synthesis by Suzuki Coupling and Residual Palladium Clean-up with SiliaMetS Thiol

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For uncomplicated malaria, Artemisinin is currently the first-line treatment. Unfortunately, the emergence of Artemisinin resistance calls for the development of alternative antimalarial treatments. The Novartis Institute for Tropical Diseases screened compounds to identify fast-acting molecules with a new chemotype. The new chemotype means a different mode of action compared to drugs currently used on the market, leading to activity against known mutants and no cross-resistance.

A series of compounds based on 5-aryl-2-amino-imidazothiadiazole derivatives were systematically screened. The screening assessed for: chemical stability, selectivity against human kinase, maintained or improved desirable pharmacological and safety properties, optimized physiochemical and finally Absorption, Distribution, Metabolism and Excretion properties (ADME). The compound INE963 (Figure 1) was identified as a potential antimalarial drug with the best overall profile (including plasmodium efficiency, half-life and half-maximum effective concentration).

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