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Design, synthesis and evaluation of a series of 5-methoxy-2,3-naphthalimide derivatives as AcrB inhibitors for the reversal of bacterial resistance.
Jin, Chaobin; Alenazy, Rawaf; Wang, Yinhu; Mowla, Rumana; Qin, Yinhui; Tan, Jin Quan Eugene; Modi, Natansh Deepak; Gu, Xinjie; Polyak, Steven W; Venter, Henrietta; Ma, Shutao.
Afiliação
  • Jin C; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China; Department of Medical Laboratory, College of Applied Medical Sciences - Shaqra, Shaqra University, 11961,
  • Alenazy R; School of Pharmacy and Medical Sciences, University of South Australia, SA 5000, Australia; Department of Medical Laboratory, College of Applied Medical Sciences - Shaqra, Shaqra University, 11961, Saudi Arabia.
  • Wang Y; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China.
  • Mowla R; School of Pharmacy and Medical Sciences, University of South Australia, SA 5000, Australia.
  • Qin Y; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China.
  • Tan JQE; School of Pharmacy and Medical Sciences, University of South Australia, SA 5000, Australia.
  • Modi ND; School of Pharmacy and Medical Sciences, University of South Australia, SA 5000, Australia.
  • Gu X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China.
  • Polyak SW; School of Pharmacy and Medical Sciences, University of South Australia, SA 5000, Australia.
  • Venter H; School of Pharmacy and Medical Sciences, University of South Australia, SA 5000, Australia. Electronic address: rietie.venter@unisa.edu.au.
  • Ma S; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China. Electronic address: mashutao@sdu.edu.cn.
Bioorg Med Chem Lett ; 29(7): 882-889, 2019 04 01.
Article em En | MEDLINE | ID: mdl-30755336
A series of novel 5-methoxy-2,3-naphthalimide derivatives were designed, synthesized and evaluated for their biological activities. In particular, the ability of the compounds to synergize with antimicrobials, to inhibit Nile Red efflux, and to target AcrB was assayed. The results showed that the most of the tested compounds more sensitized the Escherichia coli BW25113 to the antibiotics than the parent compounds 7c and 15, which were able to inhibit Nile Red efflux. Significantly, compound A5 possessed the most potent antibacterial synergizing activity in combination with levofloxacin by 4 times and 16 times at the concentration of 8 and 16 µg/mL, respectively, whilst A5 could effectively abolish Nile Red efflux at 100 µM. Additionally, target effect of A5 was confirmed in the outer- or inner membrane permeabilization assays. Therefore, A5 is an excellent lead compound for further structural optimization.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Proteínas de Escherichia coli / Proteínas Associadas à Resistência a Múltiplos Medicamentos / Farmacorresistência Bacteriana / Escherichia coli / Naftalimidas / Antibacterianos Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Proteínas de Escherichia coli / Proteínas Associadas à Resistência a Múltiplos Medicamentos / Farmacorresistência Bacteriana / Escherichia coli / Naftalimidas / Antibacterianos Idioma: En Ano de publicação: 2019 Tipo de documento: Article