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Synthesis and antibacterial activities of 7-{4-[2-[2-substituted-4- ( (5S) -5-acetylaminomethyl-2-oxo-oxazolidin-3-yl) }-phenyl] -ethyl]-piperazin-1-yl}-fluoroquinolones

Yu, H-Jie.; Zhou, W-Cheng.

Yao Xue Xue Bao 41(10): 990-999

2006

ISSN/ISBN: 0513-4870
PMID: 17184119
Document Number: 603588
To find out new oxazolidinone-fluoroquinolone derivatives with high antibacterial activity. Some 7-{4-[2-[2-substituted-4-((5S)-5- acetylaminomethyl-2-oxo-oxazolidin-3-yl)-phenyl]-ethyl]-piperazin-1-yl}-fluoroquinolones were designed and synthesized, and their antibacterial activities were tested in vitro. Twenty target compounds were obtained and their structures were confirmed by 1H NMR and MS. The target compounds had high antibacterial activities in vitro, especially, the activity of compound 22 against Enterococcus faecium was 16-fold and 64-fold more potent than that of linezolid and norfloxacin, respectively, and its MIC value against Staphylococcus aureus was 4-fold lower than that of linezolid. The oxazolidinone-fluoroquinolone derivatives improved the antibacterial activities.

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Li, R.-P.; Zhou, W.-C.; Zhou, W.-L. 2006: Synthesis and antibacterial activity of (S) -5-acetylaminomethyl-3-[(4-substituted-aminomethyl) phenyl] -2-oxazolindinone derivatives Yao Xue Xue Bao 41(5): 418-425
Islam, M.; Siddiqui, A.A. 2010: Synthesis, antituberculostatic, antifungal and antibacterial activities of 3-substituted phenyl-6-substituted phenyl-1,2,4-triazolo[4,3-b]pyridazines Acta Poloniae Pharmaceutica 67(5): 555-562
Zhou, Y.J.; Zhang, W.N.; Lu, J.G.; Li, K.; Zhu, J. 1997: Synthesis and antifungal activities of 1-(2-[(substituted-phenyl) methyl]thio)-2-(2,4-difluorophenyl)ethyl-1H-1,2,4-triazoles Yao Xue Xue Bao 32(12): 902-907
Yan, L.; Xu, B.; Ma, Z.; Zhu, Y.; Yang, Q. 1998: Synthesis and antibacterial activity of 7-substituted-1-ethyl(2-fluoro-ethyl)-6,8-difluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid Yao Xue Xue Bao 33(5): 392-395
Bedi, P.; Mahajan, M.P.; Kapoor, V.K. 2003: Synthesis and antibacterial evaluation of 4-substituted-2-phenyl-1-p-tolyl-4-thiomethyl-1,3-diazabuta-1,3-dienes: a novel class of antibacterial agents PDA Journal of Pharmaceutical Science and Technology 57(2): 109-113
Diurno, M.V.; Cristinziano, A.; Mazzoni, O.; Piscopo, E.; Bolognese, A. 1995: Synthesis and antimicrobial activity of 1-(p-substituted)phenyl-3-(p-alkoxy)phenyl-4-phenyl-azetidin-2-ones Farmaco 50(2): 143-148
El-Hadri, A.; Nicolle, E.; Leclerc, G.; Pietri-Rouxel, F.; Strosberg, A.D.; Archimbault, P. 2003: New series of N-substituted phenyl ketone oxime ethers: synthesis and bovine beta3-adrenergic agonistic activities Die Pharmazie 58(1): 13-17
Xin, T.; Ding, J.; Zhang, X.P. 1993: Synthesis and antibacterial activities of 1-amino-6-fluoro-1,4-dihydro-4-oxo-7-(substituted) piperazinyl-3-quinolinecarboxylic acids and their derivatives Yao Xue Xue Bao 28(11): 865-869
Ersan, S.; Nacak, S.; Acar, N.; Noyanalpan, N. 1997: Synthesis and antimicrobial activity of 1-dialkylaminomethyl- 2-(p-substituted phenyl)-5-substituted benzimidazole derivatives Arzneimittel-Forschung 47(4): 410-412
Bahekar, S.S.; Shinde, D.B. 2003: Synthesis and anti-inflammatory activity of some [2-amino-6-(4-substituted aryl)-4-(4-substituted phenyl)-1,6-dihydropyrimidine-5-yl]-acetic acid derivatives Acta Pharmaceutica 53(3): 223-229
Meng, X.Y.; Zhang, X.P.; Chen, X.H.; Yu, A.Z. 1991: Synthesis and antibacterial as well as antineoplastic activities of 2,4-diamino-5-methyl-6-(N-methyl-substituted benzyl) aminoquinazolines Yao Xue Xue Bao 26(5): 383-386
Li, R.L.; Zhang, W.S.; Wang, J.C.; Poe, M. 1987: Structure-activity relationships of the inhibition of Escherichia coli dihydrofolate reductase (MB1428) by 5-(substituted phenyl) thio and 5-(substituted phenyl) seleno-2,4-diaminopyrimidines Yao Xue Xue Bao 22(3): 233-237
Sánchez-Alonso, R.M.; Raviña, E.; Santana, L.; García-Mera, G.; Sanmartín, M.; Baltar, P. 1989: Piperazine derivatives of benzimidazole as potential anthelmintics. Part 1: Synthesis and activity of methyl-5-(4-substituted piperazin-1-yl)benzimidazole-2-carbamates Die Pharmazie 44(9): 606-607
Németh, G.áb.; Varga, Z.án.; Greff, Z.án.; Kéri, G.ör.; Orfi, L.ás.ó 2010: Synthesis of 4-Chloro-6-(substituted-phenyl)-pyrimidines Acta Pharmaceutica Hungarica 80(3): 101-108
Bruno, O.; Ranise, A.; Bondavalli, F.; Schenone, P.; D'Amico, M.; Filippelli, A.; Filippelli, W.; Rossi, F. 1993: 3,5-diphenyl-1H-pyrazole derivatives. XI. N-aryl-5(3)-phenyl-4-(3,5- diphenyl-1-pyrazolyl)-3(5)-pyrazole amines, 5-substituted 4,5-dihydro-3-phenyl-4-(3,5-diphenyl-1-pyrazolyl)-1H-pyrazoles and 2,6-disubstituted 1,6-dihydro-4- phenyl-5-(3,5-diphenyl-1-pyrazolyl)pyrimidines with antipyretic, antiinflammatory and other activities Farmaco 48(7): 949-966
Krishnan, S.K.; Ganguly, S.; Veerasamy, R.; Jan, B. 2011: Synthesis, antiviral and cytotoxic investigation of 2-phenyl-3-substituted quinazolin-4(3H)-ones European Review for Medical and Pharmacological Sciences 15(6): 673-681
Bhat, M.A.; Al-Omar, M.A.; Siddiqui, N. 2011: Synthesis of 2-(substituted phenyl)-3-[5-(2-oxo-2H-chromen-3-yl)-1,3,4-oxadiazol-2-yl]-1,3-thiazolidin-4-ones with antimicrobial activity Acta Poloniae Pharmaceutica 68(2): 295-299
Wujec, M.; Pitucha, M.; Dobosz, M. 2004: Synthesis of 1-substituted-4-ethyl-3-(pyridin-3-yl)-1,2,4-triazoline-5-thione Acta Poloniae Pharmaceutica 61 Suppl: 13-15
Corelli, F.; Massa, S.; Stefancich, G.; Artico, M.; Panico, S.; Simonetti, N. 1984: Researches on antibacterial and antifungal agents. Ii - Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid, a novel highly active, broad-spectrum antibacterial agent related to piromidic acid Il Farmaco; Edizione Scientifica 39(2): 95-109
Ali, M.A.; Ismail, R.; Choon, T.S.; Yoon, Y.K.; Wei, A.C.; Pandian, S.; Samy, J.G.; De Clercq, E.; Pannecouque, C. 2011: Synthesis and anti-HIV activity of novel 3-substituted phenyl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues Acta Poloniae Pharmaceutica 68(3): 343-348