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Towards eradicating antibiotic-resistant bacteria:synthesis and antibacterial activities of substituted N-(2-nitrophenyl)pyrrolidine-and piperidine-2-carboxylic acids

《中国药学:英文版》2019年 第10期 | Jocelyn A.Odusami Monisola I.Ikhile Marthe C.D.Fotsing Idris A.O.lasupo Josephat U.Izunobi Elizabeth O.Bamgbade Thierry Y.Fonkui Olayinka T.Asekun Oluwole B.Familoni Derek T.Ndinteh   Department of Chemical Sciences Yaba College of Technology Yaba Lagos Nigeria Department of Applied Chemistry P.O Box 17011 Doornfontein Campus 2028 University of Johannesburg South Africa Department of Chemistry University of Lagos Akoka Lagos Nigeria Department of Biotechnology and Food Technology P.O Box 17011 Doornfontein Campus 2028 University of Johannesburg South Africa
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摘 要:Antibacterial resistance is a source of great concern in the effective prevention and treatment of infections caused by bacteria,making the development of requisite therapeutics a major challenge.N-(Nitrophenyl)cycloamino acids are important compounds in the synthesis of poly-condensed nitrogen-containing heterocycles with marked activities in many biological systems.A series of substituted N-(o-nitrophenyl)cycloamino-2-carboxylic acids 3a–3g were synthesized via the condensation reaction of substituted o-halogenonitrobenzenes with L-proline 2a and D,L-pipecolinic acid 2b,under refluxing alcoholic basic conditions in excellent yields.The synthesized compounds were characterised by FT-IR,(1H&13C)NMR,UV-Vis,mass spectroscopy and elemental analysis.Their antibacterial activities were evaluated against five Gram-positive and five Gram-negative bacterial strains using the broth micro-dilution procedure.The antibacterial activities of the synthesized compounds were compared with streptomycin and nalidixic acid as standard antibiotic drugs.The minimum inhibitory concentration(MIC)values of compounds 3a–3g revealed good antibacterial activities against the tested microorganisms.Compounds 3a–3g were more potent than nalidixic acid against Enterococcus faecalis,Mycobacterium smegmatis,Escherichia coli and Proteus vulgaris and also more potent than streptomycin against Enterobacter cloacae and Staphylococcus aureus.Compounds 3a,3c and 3g displayed the highest antibacterial potency with an MIC value of 15.6μg/mL against E.cloacae,E.faecalis and P.mirabilis,respectively.These results indicated that these aryl cycloamino acids with antibacterial activities had potential applications as substitutes for antimicrobial peptide antibiotics,which are not susceptible to bacterial resistance,to solve the problem of drug resistance.
【分 类】【医药、卫生】 > 药学 > 药物基础科学 > 药物化学
【关键词】 ANTIBIOTICS Bacteria Cyclic amino acids o-Halogenonitrobenzene
【出 处】 《中国药学:英文版》2019年 第10期 704-715页 共12页
【收 录】 中文科技期刊数据库

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