New N-Substituted Maleimide Drug Polymers: Synthesis, Drug Release and Antibacterial Activity

Dhuha Kashash, M. Kareem, Naser Naser
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Abstract

In this work, new substituted drugs polymerized as new homogenous polymers with study their medicinal properties to extend the controlled drug. The first step includes the preparation of compound N-(4 - hydroxyphenyl) maleimide (D 1 ) via a reaction of maleic anhydride with 4-aminophenol. Then compound (D 1 ) was converted to maleimide phenol acetic acid ether (D 2 ) which converted to its corresponding acyl chloride derivative which reacted with amino drugs (Ceftriaxone, Ciprofloxacin) afforded monomers (D 3 and D 4 ). Homogeneous polymers (D 5 and D 6 ) were prepared via free radical polymerization reaction of the monomers (D 3 , and D 4 ) under nitrogen using Benzoyl peroxide (Bpo) as initiator. All these prepared monomers and polymers were characterized by FT-IR and 1 H-NMR, 13 C-NMR techniques and C.H.N.S . Study of the drug release behavior in acidic and basic media as well as the swelling ratio were achieved. The antibacterial activity and physical properties of all monomers and polymers were studied.
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新型 N-取代马来酰亚胺药物聚合物:合成、药物释放和抗菌活性
在这项工作中,新的替代药物聚合成了新的均质聚合物,并研究了它们的药用特性,以扩大受控药物的范围。第一步包括通过马来酸酐与 4-氨基苯酚的反应制备化合物 N-(4-羟基苯基)马来酰亚胺(D 1)。然后将化合物(D 1 )转化为马来酰亚胺苯乙醇醚(D 2 ),再转化为相应的酰基氯衍生物,与氨基药物(头孢曲松、环丙沙星)反应生成单体(D 3 和 D 4 )。在氮气环境下,以过氧化苯甲酰(Bpo)为引发剂,通过单体(D 3 和 D 4)的自由基聚合反应制备均相聚合物(D 5 和 D 6)。所有这些制备的单体和聚合物都通过傅立叶变换红外光谱、1 H-NMR 和 13 C-NMR 技术以及 C.H.N.S 进行了表征。研究了药物在酸性和碱性介质中的释放行为以及溶胀率。研究了所有单体和聚合物的抗菌活性和物理性质。
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