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Recently, by using previously described EPIs, we developed pharmacophore models able to identify inhibitors of NorA, the most studied efflux pump of <jats:italic>Staphylococcus aureus<\/jats:italic>. Herein we report the pharmacophore\u2010based virtual screening of a library of new potential NorA EPIs generated by an <jats:italic>in\u2010silico<\/jats:italic> scaffold hopping approach of the quinoline core. After chemical synthesis and biological evaluation of the best virtual hits, we found the quinazoline core as the best performing scaffold. Accordingly, we designed and synthesized a series of functionalized 2\u2010arylquinazolines, which were further evaluated as NorA EPIs. 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