Fig. 1: Structure-Activity Relationship (SAR) leading to the selection of BWC0977 as the clinical candidate.
From: BWC0977, a broad-spectrum antibacterial clinical candidate to treat multidrug resistant infections
The synthesis of the screening hit, compound 1 and the progressive synthesis of different compounds based on medicinal chemistry inputs towards improving the compound properties. The latter included enhanced potency, broad-spectrum antibacterial activity, optimal physico-chemical properties while mitigating tox liability leading to the selection of the clinical candidate, compound 9 or BWC0977. Abbreviations: Eco, Escherichia coli; Pae, Pseudomonas aeruginosa; Aba, Acinetobacter baumannii; Kpn, Klebsiella pneumoniae.
