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Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-12-01 00:00:00 , DOI: 10.1039/c7md00527j G M L Consoli 1 , G Granata 1 , R Picciotto 2 , A R Blanco 3 , C Geraci 1 , A Marino 4 , A Nostro 4
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-12-01 00:00:00 , DOI: 10.1039/c7md00527j G M L Consoli 1 , G Granata 1 , R Picciotto 2 , A R Blanco 3 , C Geraci 1 , A Marino 4 , A Nostro 4
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The growing antibiotic resistance phenomenon continues to stimulate the search for new compounds and strategies to combat bacterial infections. In this study, we designed and synthesized a new polycationic macrocyclic compound (2) bearing four N-methyldiethanol ammonium groups clustered and circularly organized by a calix[4]arene scaffold. The in vitro activity of compound 2, alone and in combination with known antibiotics (ofloxacin, chloramphenicol or tetracycline), was assessed against strains of Staphylococcus aureus (ATCC 6538 and methicillin-resistant isolate 15), S. epidermidis (ATCC 35984 and methicillin-resistant isolate 57), and Pseudomonas aeruginosa (ATCC 9027 and antibiotic-resistant isolate 1). Calix[4]arene derivative 2 showed significant antibacterial activity against ATCC and methicillin-resistant Gram positive Staphylococci, improved the stability of tetracycline in water, and in combination with antibiotics enhanced the antibiotic efficacy against Gram negative P. aeruginosa by an additive effect.
中文翻译：
聚阳离子杯[4]芳烃衍生物单独以及与抗生素组合的设计、合成和抗菌评估†
日益增长的抗生素耐药性现象继续刺激人们寻找新的化合物和对抗细菌感染的策略。在这项研究中，我们设计并合成了一种新的聚阳离子大环化合物（2），其带有四个N-甲基二乙醇铵基团，通过杯[4]芳烃支架聚集并环状组织。化合物2单独以及与已知抗生素（氧氟沙星、氯霉素或四环素）组合的体外活性针对金黄色葡萄球菌菌株（ATCC 6538 和甲氧西林抗性分离株 15）、表皮葡萄球菌菌株（ATCC 35984和甲氧西林）进行了评估。耐药分离株 57) 和铜绿假单胞菌(ATCC 9027 和抗生素耐药分离株 1)。Calix[4]芳烃衍生物2对ATCC和耐甲氧西林革兰氏阳性葡萄球菌表现出显着的抗菌活性，提高了四环素在水中的稳定性，与抗生素合用可通过相加作用增强对革兰氏阴性铜绿假单胞菌的抗菌功效。
更新日期：2017-12-01
中文翻译：
聚阳离子杯[4]芳烃衍生物单独以及与抗生素组合的设计、合成和抗菌评估†
日益增长的抗生素耐药性现象继续刺激人们寻找新的化合物和对抗细菌感染的策略。在这项研究中，我们设计并合成了一种新的聚阳离子大环化合物（2），其带有四个N-甲基二乙醇铵基团，通过杯[4]芳烃支架聚集并环状组织。化合物2单独以及与已知抗生素（氧氟沙星、氯霉素或四环素）组合的体外活性针对金黄色葡萄球菌菌株（ATCC 6538 和甲氧西林抗性分离株 15）、表皮葡萄球菌菌株（ATCC 35984和甲氧西林）进行了评估。耐药分离株 57) 和铜绿假单胞菌(ATCC 9027 和抗生素耐药分离株 1)。Calix[4]芳烃衍生物2对ATCC和耐甲氧西林革兰氏阳性葡萄球菌表现出显着的抗菌活性，提高了四环素在水中的稳定性，与抗生素合用可通过相加作用增强对革兰氏阴性铜绿假单胞菌的抗菌功效。
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