• 专利标题:   Improving antibacterial activity and biocompatibility of surface of substrate, comprises e.g. providing at least part of surface of substrate, pre-activating, and contacting polymer segment acetamide compounds with pre-activated surface.
  • 专利号:   CN113185740-A
  • 发明人:   LIU R, WU Y
  • 专利权人:   UNIV EAST CHINA SCI TECHNOLOGY
  • 国际专利分类:   A61L015/46, A61L027/54, A61L031/16, C03C017/34, C08J007/04, C08J009/42, C08L061/16, C08L075/04
  • 专利详细信息:   CN113185740-A 30 Jul 2021 C08J-007/04 202174 Pages: 39 Chinese
  • 申请详细信息:   CN113185740-A CN10476700 29 Apr 2021
  • 优先权号:   CN10476700

▎ 摘  要

NOVELTY - Improving antibacterial activity and biocompatibility of surface of substrate, comprises (i) providing at least a part of surface of substrate, (ii) pre-activating at least a part of surface so that the surface has reactive group including -NH2, -Br, -Cl, -OH, -COOH, -C(=O)H, epoxy groups, oxygen radicals, alkenyl groups, alkynyl groups, polydopamine composite layers, or combinations to obtain pre-activated surface, and (iii) contacting and reacting compound or its salt with pre-activated surface to obtain at least a part of surface having antibacterial activity and biocompatibility of the substrate, where compound comprises polymer segment i.e. acetamide compounds (I)-(III). USE - The substrate is useful for preparing products having improved antibacterial activity and biocompatibility (claimed); and in the field of biomedical materials, preventing and treating microbial surface infections. ADVANTAGE - The substrate: utilizes modified functional surface which has high antibacterial activity against gram-negative bacteria and/or gram-positive bacteria and/or fungi; and has low hemolytic activity on red blood cells, excellent cell compatibility to mammalian cells, and negligible toxicity for long-term antibacterial activity after implantation in the body. DETAILED DESCRIPTION - Improving antibacterial activity and biocompatibility of surface of substrate, comprises (i) providing at least a part of surface of the substrate, (ii) pre-activating at least a part of surface so that the surface has reactive group including -NH2, -Br, -Cl, -OH, -COOH, -C(=O)H, epoxy groups, oxygen radicals, alkenyl groups, alkynyl groups, polydopamine composite layers, or combinations to obtain pre-activated surface, and (iii) contacting and reacting compound or its salt with pre-activated surface to obtain at least a part of surface having antibacterial activity and biocompatibility of the substrate, where compound comprises polymer segment i.e. acetamide compounds of formulae (I)-(III). R1, R2 and R3 = -L1Ra, H, halo, -OH, -COOH, 1-15C alkyl, 2-15C alkenyl, 2-15C alkynyl, or optionally substituted 3-12C cycloalkyl; L1 = bond, optionally substituted 1-8C alkylene, 2-8C alkenylene or 2-8C alkynylene; Ra = -NRbRb, guanidine group, biguanide, or N(Rb)3+; -L1Ra = -2-6C alkyl-Ra, preferably, -3-6C alkyl-Ra; R4, R5 and R6 = H, halo, -OH, -COOH, optionally substituted 1-15C alkyl, 2-15C alkenyl, 2-15C alkynyl, 3-12C cycloalkyl, benzyl, phenyl, 5-10 membered heteroaryl including 1-3 heteroatoms O, N, S, 1-6C alkyl-Rc, or 1-6C alkyl-COO-Rc; Rc = 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, optionally substituted benzyl, phenyl, 3-12C cycloalkyl group and 5-10 membered heteroaryl group including 1-3 heteroatoms O, N, and S; R4 and R5 and the connected carbon atoms = form optionally substituted 3-12C cycloalkyl group; x = 5-100; x+y = 100; n = 1-100; R7-R15 = H, halo, -OH, -COOH, optionally substituted 1-15C alkyl, 2-15C alkenyl, 2-15C alkynyl, 3-12C cycloalkyl or two substituent's on adjacent or same carbon atom form optionally substituted 3-12C cycloalkyl group with connected carbon atom; R11, R17 = L1Ra; R16 = H, -OH, optionally substituted 1-15C alkyl, 2-15C alkenyl, 2-15C alkynyl, 1-15C alkoxy, 3-12C cycloalkyl, 1-6C alkyl-3-12C cycloalkyl, benzyl, phenyl group, 5-10 membered heteroaryl group including 1-3 heteroatoms O, N, and S, or optionally substituted 1-6C alkyl-Rc, or 1-6C alkyl-COO-Rc; R18 = H, halo, -OH, -COOH, optionally substituted 1-15C alkyl, 2-15C alkenyl, 2-15C alkynyl, 3-12C cycloalkyl, benzyl, phenyl, 5-10 membered heteroaryl including 1-3 heteroatoms O, N, S, 1-6C alkyl-Rc, or 1-6C alkyl-COO-Rc; Rb = optionally substituted hydrogen, 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, or two Rb on the same N atom and connected N atom form 4-8 membered heterocyclic group containing one N atom; and ubstitution = H on each group is substituted by group including deuterium, halo, -SH, -COOH, -OH, -NH2, benzyl, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 1-6C alkoxy, 1-6C haloalkyl, 1-6C haloalkoxy, 2-6C haloalkenyl, 2-6C haloalkynyl, 3-8C cycloalkyl or 6-10C aryl. An INDEPENDENT CLAIM is also included for substrate with at least a portion of surface having improved antibacterial activity and biocompatibility and product containing or prepared from substrate, comprising at least a part of surface having improved antibacterial activity and biocompatibility.