Synthesis of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1, 2, 4-triazines that have antibacterial activity and also inhibit inorganic pyrophosphatase

…, KL Molland, MN Seleem, A Ghafoor, MI Hamed…

Index: Lv, Wei; Banerjee, Biplab; Molland, Katrina L.; Seleem, Mohamed N.; Ghafoor, Adil; Hamed, Maha I.; Wan, Baojie; Franzblau, Scott G.; Mesecar, Andrew D.; Cushman, Mark Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 1 p. 406 - 418

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Citation Number: 14

Abstract

Abstract Inorganic pyrophosphatases are potential targets for the development of novel antibacterial agents. A pyrophosphatase-coupled high-throughput screening assay intended to detect o-succinyl benzoic acid coenzyme A (OSB CoA) synthetase inhibitors led to the unexpected discovery of a new series of novel inorganic pyrophosphatase inhibitors. Lead optimization studies resulted in a series of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1, 2, 4-triazine ...