Synthesis and bioactivity of novel ester derivatives of rhein / 中国药学杂志

ABSTRACT

OBJECTIVE: To design and synthesize a series of novel ester derivatives of rhein were designed and synthesized, and evaluate their anti-MRSA activity. METHODS: The title compounds were synthesized with rhein and α-hydroxyphosphonate as starting materials, EDCI/HOBT and [Bmim] BF4 as catalyst system. And the anti-MRSA activities of the products were evaluated by the agar dilution method. RESULTS: Ten title compounds were synthesized,and their structures were clearly established by IR, NMR and MS. The RESULTS: showed that the derivatives have different anti-MRSA activity. Especially, showed potent activity against MRSA with the minimum inhibitory concentration(MIC) and minimum bactericidal concentration(MBC) values of compound Ⅱ-3 was 128, 512 μg·mL-1 respectively,superior to rhein and oxacillin. And the MIC and MBC of compound Ⅱ-10 to MRSA was 32, 64 μg·mL-1, its anti-MRSA activity was obviously better than that of rhein and oxacillin. CONCLUSION: The ester derivatives of rhein are significant resistant to MRSA, which is worth for further study.