Kim, nam kyoung Sandip, Sengupta Lee, Jiwon Uttam, Dash Kim, Soojeung 김학중 Song, Chiman 심태보 2024-01-12T06:33:08Z 2024-01-12T06:33:08Z 2023-07-12 2023-11 0223-5234 https://pubs.kist.re.kr/handle/201004/79784 SbnE is an essential enzyme for staphyloferrin B biosynthesis in Staphylococcus aureus. An earlier study showed that natural product baulamycin A has in vitro inhibitory activity against SbnE and antibacterial potency. A SAR study with analogues of baulamycin A was conducted to identify potent inhibitors of SbnE and/or effective antibiotics against MRSA. The results show that selected analogues, including 11, 18, 21, 24a, 24c, 24m and 24n, exhibit single-digit micromolar inhibitory potencies against SbnE (IC50s = 1.81？8.94 μM) and 11, 24m, 24n possess significant activities against both SbnE (IC50s = 4.12？6.12 μM) and bacteria (MICs = 4？32 μg/mL). Biological investigations revealed that these substances possess potent cell wall disruptive activities and that they inhibit siderophore production in MRSA. Among the selected analogues, 7 has excellent antibiotic activities both gram-positive and ？negative bacteria (0.5？4 μg/mL). Moreover, these analogues significantly impede biofilm formation in a concentration-dependent manner. Taken together, the results of the investigation provide valuable insight into the nature of novel baulamycin A analogues that have potential efficacy against MRSA owing to their membrane damaging activity and/or inhibitory efficacy against siderophore production. English Elsevier BV Synthesis and antibacterial activities of baulamycin A inspired derivatives Article 10.1016/j.ejmech.2023.115592 1 European Journal of Medicinal Chemistry, v.259 European Journal of Medicinal Chemistry 259 N scie scopus 001149482300001 Chemistry, Medicinal Pharmacology & Pharmacy Article RESISTANT STAPHYLOCOCCUS-AUREUS STEREOSELECTIVE-SYNTHESIS CHEMICAL-SYNTHESIS VIRULENCE IRON INFECTIONS ANTIBIOTICS SIDEROPHORE ALCOHOLS BIOSYNTHESIS Baulamycin A SbnE Siderophore Methicillin-resistant Staphylococcus aureus (MRSA)