A series of semisynthetic triterpenoids with A-ring azepano- and A-seco-fragments as well as hydrazido/hydrazono-substituents at C3 and C28 has been synthesized and evaluated for antimicrobial activity against key ESKAPE pathogens and DNA viruses (HSV-1, HCMV, HPV-11). It was found that azepanouvaol 8, 3-amino-3,4-seco-4(23)-en derivatives of uvaol 21 and glycyrrhetol-dien 22 as well as azepano-glycyrrhetol-tosylate 32 showed strong antimicrobial activities against MRSA with MIC ≤ 0.15 μM that exceeds the effect of antibiotic vancomycin. Azepanobetulinic acid cyclohexyl amide 4 exhibited significant bacteriostatic effect against MRSA (MIC ≤ 0.15 μM) with low cytotoxicity to HEK-293 even at a maximum tested concentration of >20 μM (selectivity index SI 133) and may be considered a noncytotoxic anti-MRSA agent. Azepanobetulin 1, azepanouvaol 8, and azepano-glycyrrhetol 15 showed high potency towards HCMV (EC₅₀ 0.15; 0.11; 0.11 µM) with selectivity indexes SI₅₀ 115; 136; 172, respectively. The docking studies suggest the possible interactions of the leading compounds with the molecular targets.

一系列半合成三萜类化合物在 C3 和 C28 具有 A 环氮杂和 A-seco 片段以及酰肼基/亚肼基取代基，已合成并评估了对关键 ESKAPE 病原体和 DNA 病毒（HSV-1、HCMV）的抗菌活性, HPV-11). 结果发现，azepanouvaol 8 、uvaol 21和 glycyrrhetol-dien 22的 3-amino-3,4-seco-4(23)-en 衍生物以及 azepano-glycyrrhetol-tosylate 32对 MRSA 具有很强的抗菌活性，MIC ≤ 0.15 μM，超过抗生素万古霉素的作用。氮杂白桦酸环己基酰胺4对 MRSA（MIC ≤ 0.15 μM）表现出显着的抑菌作用，对 HEK-293 具有低细胞毒性，即使在最大测试浓度 > 20 μM（选择性指数 SI 133）时也是如此，可以被认为是一种无细胞毒性的抗 MRSA 药物。Azepanobetulin 1、azepanouvaol 8和 azepano-glycyrrhetol 15显示出对 HCMV 的高效力（EC ₅₀ 0.15；0.11；0.11 µM），选择性指数 SI ₅₀ 115；136; 分别为 172。对接研究表明先导化合物与分子靶标可能存在相互作用。