数字农科院2.0

An Efficient Novel Synthesis Of 1.4-O-[(4-Amino-6-Hydroxy-Pyrimidine-2-Yl)Thioacetyl]Mutilin And The Antibacterial E valuation

文献类型: 外文期刊

作者: Shang Ruo-Feng;Xu Wen-Jun;Yi Yun-Peng;Huang Xin;Xu Wen-Jun;Liang Jian-Ping

作者机构:

关键词: pleuromutilin; single-crystal structure; antibacterial activities

期刊名称: CHINESE JOURNAL OF STRUCTURAL CHEMISTRY

ISSN: 0254-5861

年卷期: 2017 年 36 卷 9 期

页码:

摘要: The title structure of 14-O-[(4-amino-6-hydroxy-pyrimidine-2-yl)thioacetyl]mutilin, C26H47N3O5S, has been synthesized using 22-O-tosyl pleuromutilin and 4-amine-6-hydroxy-2-mercatopyrimidine monohydrate, and its structure was characterized by IR, NMR, H RMS and single-crystal X-ray diffraction. This compound has a 5-6-8 tricyclic carbon skeleton and a pyrimidine ring. It crystallizes in orthorhombic, space group P2(1)2(1)2(1) with a = 10.494(3), b = 16.997(5), c = 16.997 angstrom, Z = 4, D-c = 1.275 Mg.m(-3), mu = 0.220 mm(-1), F(000) = 1248, wR(F-2) = 0.1159 and R = 0.0381. The preliminary biological test showed that the title compound has more potent inhibitions to Staphylococcus aureus, MRSA and MRSE than that of tiamulin fumarate in vitro.

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