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Azoles are first-line drugs used in fungal infections. Topical antifungals, such as miconazole and econazole, are known to be active against Gram-positive bacteria, which was reported to result from bacterial flavohemoglobin (flavoHb) inhibition. Dual antibacterial/antifungal action is believed to have benefits for antimicrobial chemotherapy. In this study, we tested antibacterial effects of an in-house library of naphthalene-bearing azoles, some of which were reported as potent antifungals, in an attempt to find dual-acting hits. Several potent derivatives were obtained against the Gram-positive bacteria,  Enterococcus faecalis  and  Staphylococcus aureus .  9  was active at a minimum inhibitor concentration (MIC) less than 1 µg/ml against  E. faecalis  and  S. aureus , and  10  against  S. aureus .  16  was also potent against  E. faecalis  and  S. aureus  (MIC = 1 and 2 µg/ml, respectively). Six more were active against  S. aureus  with MIC ≤ 4 µg/ml.  In vitro  cytotoxicity studies showed that the active compounds were safe for healthy cells within their MIC ranges. According to the calculated descriptors, the library was found within the drug-like chemical space and free of pan-assay interference compounds (PAINS). Molecular docking studies suggested that the compounds might be bacterial flavohemoglobin (flavoHb) inhibitors and the azole and naphthalene rings were important pharmacophores, which was further supported by pharmacophore modeling study. As a result, the current study presents several non-toxic azole derivatives with antibacterial effects. In addition to their previously reported antifungal properties, they could set a promising starting point for the future design of dual acting antimicrobials. Communicated by Ramaswamy H. Sarma

journal of biomolecular structure and dynamics

Azoles containing naphthalene with activity against Gram-positive bacteria:  in vitro  studies and  in silico  predictions for flavohemoglobin inhibition