Isorhoifaundecanol derivatives, methods of making and antibacterial applications thereof
By modifying the structure of isosaflavin, the Mannich base derivative 12p was synthesized, which solved the problem of weakened efficacy of existing antibiotics against MRSA and realized the development of antibacterial drugs with high bactericidal efficiency and good in vivo safety.
Patent Information
- Application Number
- CN202610589910.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-04-30
- Publication Date
- 2026-07-17
AI Technical Summary
Existing antibiotics are less effective against methicillin-resistant Staphylococcus aureus (MRSA), necessitating the development of novel antibacterial drugs with novel skeletal structures and unique mechanisms of action. The physicochemical properties of isosaflavin limit its direct application as a clinical candidate drug.
Using isosaflavin as a lead compound, a series of Mannich base derivatives were synthesized by reacting with aldehydes and piperidines or alkane amines/heterocyclic amines with different aromatic substitutions. The preferred compound 12p was introduced to introduce a hydrophilic alicyclic amine side chain, thereby regulating the physicochemical properties of the molecule to enhance its antibacterial activity.
The synthesized derivative 12p significantly enhances in vitro antibacterial activity by targeting and disrupting bacterial cell membranes, while also exhibiting excellent in vivo therapeutic effects and biosafety, and is less likely to induce drug resistance, thus possessing potential clinical application value.
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Figure CN122404255A_ABST