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Structure-based scaffold modification and CADD-guided optimization campaign that culminated in the discovery of compound 65, with improved pharmacokinetic properties, leading to enhanced in vivo efficacy compared to levofloxacin in a murine infection model Ying Fu, Yushe Yang et al Overcoming hERG inhibition in antibacterial GP-1 ATPase inhibitors Overcoming the associated hERG inhibition and suboptimal PK profiles associated with otherwise potent and broad-spectrum antibacterial active (MDR Gram-positive & Gram-negative pathogens) pyrimido[4,5-b]indole based (GP-1) ATPase inhibitors of DNA gyrase, the publication reports

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