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Synthesis and Antibacterial Activities of New Oxazolidinone Compounds

Author: HaoJinHeng
Tutor: GongPing
School: Shenyang Pharmaceutical University
Course: Medicinal Chemistry
Keywords: Antimicrobial drugs Oxazolidinone Linezolid Design Synthesis Antibacterial activity
CLC: R96
Type: Master's thesis
Year: 2005
Downloads: 33
Quote: 0
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Abstract


This article is about the design of new antibacterial agents oxazolidinone compounds , synthesis and antibacterial activity studies . This paper describes the mechanism of action and research trends in antimicrobial details research progress of the oxazolidinone compounds and antibacterial mechanism , focusing on the design , synthesis and antibacterial activity of novel oxazolidinone compounds . Linezolid lead compound , on the basis of the analysis of the structure-activity relationship of oxazolidinone compounds , the authors retain the oxazolidinone parent ring required pharmacophore substituted ring 3 and 5 base transformation: introduced at the 3 - position 3 - fluoro -4 - (2 - methyl - thiazol -4 - yl ) phenyl , 3 - fluoro - 4 - [ 2 - ( pyridin-2 - yl ) thiazole-4 - yl ]-phenyl , 5 - introducing sulfur substituted bit methylene group and a substituted amide group , in order to find new compounds having a potential antimicrobial activity through changes in the group which may be substituted , and further exploration of the structure-activity relationship . The method according to the literature , as raw materials, inter- fluoroaniline synthesis seventeen new compounds have not been reported . Its structure was confirmed by NMR and MS. Trace liquid dilution method , determination of target compounds antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis .

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CLC: > Medicine, health > Pharmacy > Pharmacology
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