恶唑烷酮类抗菌剂的构效关系（SAR）研究。1. 恶唑烷酮5-位取代基的转化
Structure-activity relationship (SAR) studies on oxazolidinone antibacterial agents. 1. Conversion of 5-substituent on oxazolidinone.
作者信息
Tokuyama R, Takahashi Y, Tomita Y, Suzuki T, Yoshida T, Iwasaki N, Kado N, Okezaki E, Nagata O
机构信息
Research and Development Division, Hokuriku Seiyaku Co., Ltd., Katsuyama, Fukui, Japan.
出版信息
Chem Pharm Bull (Tokyo). 2001 Apr;49(4):347-52. doi: 10.1248/cpb.49.347.
A structure-activity relationship (SAR) study on 5-substituted oxazolidinones as an antibacterial agent is described. The oxazolidinones, of which 5-acetylaminomethyl moiety was converted into other functions, were prepared and evaluated for antibacterial activity. Elongation of the methylene chain (8) and conversion of the acetamido moiety into guanidino moiety (12) decreased the antibacterial activity. The replacement of carbonyl oxygen (=O) by thiocarbonyl sulfur (=S) enhanced in vitro antibacterial activity. Especially, compound 16, which had the 5-thiourea group, showed 4-8 stronger in vitro activity than linezolid. Our SAR study revealed that the antibacterial activity was greatly affected by the conversion of 5-substituent.
描述了一项关于5-取代恶唑烷酮作为抗菌剂的构效关系（SAR）研究。制备了5-乙酰氨基甲基部分转化为其他官能团的恶唑烷酮，并对其抗菌活性进行了评估。亚甲基链的延长（8）和乙酰胺基部分向胍基部分的转化（12）降低了抗菌活性。用硫代羰基硫（=S）取代羰基氧（=O）增强了体外抗菌活性。特别是，具有5-硫脲基团的化合物16在体外显示出比利奈唑胺强4-8倍的活性。我们的构效关系研究表明，5-取代基的转化对抗菌活性有很大影响。
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