Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

高等学校化学研究 ›› 2006, Vol. 22 ›› Issue (4): 459-464.

Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

ZHAI Xin, ZHAO Yan-fang, WANG Jia, HONG Wei, HUANG Liang, GONG Ping

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

收稿日期:2005-07-05 出版日期:2006-08-24 发布日期:2011-08-06

Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

ZHAI Xin, ZHAO Yan-fang, WANG Jia, HONG Wei, HUANG Liang, GONG Ping

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

Received:2005-07-05 Online:2006-08-24 Published:2011-08-06

摘要/Abstract

摘要： Sixteen novel oxazolidinone analogs containing substituted thiazole/fused-bicyclic(imidazo[1,2-b] pyridazine/imidazo[2,1-b]thiazole) groups were designed and synthesized. A new method for the preparation of the key intermediate compound 11 was proposed. The structures of the target compounds were confirmed by ¹H NMR, IR and MS, and their in vitro antibacterial activities against staphylococcus aureus were evaluated. Among them, compound 16a displays a promising antibacterial activity comparable to that of linezolid.

关键词: Oxazolidinone analog, Synthesis, Antibacterial activity

Abstract: Sixteen novel oxazolidinone analogs containing substituted thiazole/fused-bicyclic(imidazo[1,2-b] pyridazine/imidazo[2,1-b]thiazole) groups were designed and synthesized. A new method for the preparation of the key intermediate compound 11 was proposed. The structures of the target compounds were confirmed by ¹H NMR, IR and MS, and their in vitro antibacterial activities against staphylococcus aureus were evaluated. Among them, compound 16a displays a promising antibacterial activity comparable to that of linezolid.

Key words: Oxazolidinone analog, Synthesis, Antibacterial activity

ZHAI Xin, ZHAO Yan-fang, WANG Jia, HONG Wei, HUANG Liang, GONG Ping. Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups[J]. 高等学校化学研究, 2006, 22(4): 459-464.

[1]	FAN Kui, SUN Yining, XU Pengcheng, GUO Jian, LI Zhenhua, SHAO Mingfei. Single-atom Catalysts Based on Layered Double Hydroxides[J]. 高等学校化学研究, 2022, 38(5): 1185-1196.
[2]	JI Yuancheng, XU Jiayun, SUN Hongcheng, and LIU Junqiu. Artificial Photosynthesis(AP): from Molecular Catalysts to Heterogeneous Materials[J]. 高等学校化学研究, 2022, 38(3): 688-697.
[3]	CHEN Juan, WANG Jiajia, CHEN Chongan and YANG Guoyu. Two New Borates Built by Different Types of {B₉} Cluster Units[J]. 高等学校化学研究, 2022, 38(3): 744-749.
[4]	Mohammad Javad TAGHIZADEH, Maryam Saleh MOHAMMADNIA, Masoumeh GHALKHANI, Esmail SOHOULI. Improved Method for the Total Synthesis of Azaperone and Investigation of Its Electrochemical Behavior in Aqueous Solution[J]. 高等学校化学研究, 2022, 38(2): 546-551.
[5]	SUN Xiao-Shuang, QIN Dan, LI Xu-Yan, YANG Guo-Yu. A New Tubular Borate Built by[B₁₄O₂₄(OH) ₆]^12- Cluster Units[J]. 高等学校化学研究, 2022, 38(1): 123-127.
[6]	WANG Zelin, LIU Guihao, SHEN Tianyang, TAN Ling, ZHAO Yufei, SONG Yu-Fei. Remote Synthesis of Layered Double Hydroxide Nanosheets Through the Automatic Chemical Robot[J]. 高等学校化学研究, 2022, 38(1): 217-222.
[7]	ZHANG Xiaosi, YANG Miao, TIAN Peng, LIU Zhongmin. Progress in Seed-assisted Synthesis of (Silico) Aluminophosphate Molecular Sieves[J]. 高等学校化学研究, 2022, 38(1): 1-8.
[8]	LUAN Huimin, WU Qinming, ZHANG Jian, WANG Yeqing, MENG Xiangju, XIAO Feng-Shou. Sustainable Synthesis of Core-Shell Structured ZSM-5@Silicalite-1 Zeolite[J]. 高等学校化学研究, 2022, 38(1): 136-140.
[9]	FANG Yuan, HEYDARI Zahra, LIU Chenghao, ZHANG Nianyue, CUCCIA Louis A., IVASENKO Oleksandr, PEREPICHKA Dmitrii F.. Glaser Coupling of Substituted Anthracene Diynes on a Non-metallic Surface at the Vapor-Solid Interface[J]. 高等学校化学研究, 2021, 37(5): 1143-1148.
[10]	ZHAO Lei, YANG Ge, GUO Hailing, WANG Chunzheng, WANG Lijuan, Svetlana MINTOVA. Effect of Sodium Concentration on the Synthesis of Faujasite by Two-step Synthesis Procedure[J]. 高等学校化学研究, 2021, 37(5): 1137-1142.
[11]	ZHANG Ling, FU Yihong, DING Yue, MENG Jiao, WANG Zhenchao, WANG Peiyi. Antibacterial Activity of Novel 18β-Glycyrrhetinic Hydrazide or Amide Derivatives[J]. 高等学校化学研究, 2021, 37(3): 662-667.
[12]	DONG Xin, CHEN Xi, ZHOU Zhaohui. Efficient Synthesis of p-Hydroxyphenyl Ethanol from Hydrogenation of Methyl p-Hydroxyphenylacetate with CNTs-promoted Cu-Zr Catalyst[J]. 高等学校化学研究, 2021, 37(3): 745-750.
[13]	LI Yuan, LI Ruizhe, LI Zhenhua, WEI Weiqin, OUYANG Shuxin, YUAN Hong, ZHANG Tierui. Effect of Support on Catalytic Performance of Photothermal Fischer-Tropsch Synthesis to Produce Lower Olefins over Fe₅C₂-based Catalysts[J]. 高等学校化学研究, 2020, 36(6): 1006-1012.
[14]	ZHAO Yanhui, YU Haifeng, LIAO Peiqiu, WANG Wenju. Green and Efficient Synthesis of 3-Pyrazolyl Indoles in Water[J]. 高等学校化学研究, 2020, 36(5): 847-852.
[15]	WANG Lili, LIU Yanan, PENG Xiaoxing, SUN Yuanqing, LIU Xiaohua, LIU Huimin, LIN Quan, SUN Hongchen, YANG Bai, LI Xiangwei. Preparation and Characterization of CaO/ZnO Core-shell Structured Nanoparticles[J]. 高等学校化学研究, 2020, 36(5): 970-975.

Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

PDF (PC)

可视化

被引次数

摘要/Abstract

引用本文

使用本文

参考文献

相关文章 15

编辑推荐

Metrics

本文评价