Citation: YI Yun-Peng, YANG Guan-Zhou, GUO Zhi-Ting, AI Xin, SHANG Ruo-Feng, LIANG Jian-Ping. A New Pleuromutilin Derivative: Synthesis, Crystal Structure and Antibacterial Evaluation[J]. Chinese Journal of Structural Chemistry, ;2015, 34(9): 1434-1439. doi: 10.14102/j.cnki.0254-5861.2011-0750 shu

A New Pleuromutilin Derivative: Synthesis, Crystal Structure and Antibacterial Evaluation

1.
a Key Laboratory of New Animal Drug Project of Gansu Province; Key Laboratory of Veterinary Pharmaceutical Development, Ministry of Agriculture, China; Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, 335 Jiangouyan, Lanzhou 730050, China;
2.
b School of Pharmacy, Lanzhou University, Lanzhou 730020, China

Received Date: 2 April 2015
Available Online: 27 May 2015
Fund Project: Supported by Basic Scientific Research Funds in Central Agricultural Scientific Research Institutions (No.1610322014003) (No.1610322014003)

A new pleuromutilin derivative, 14-O-[(4,6-diaminopyrimidine-2-yl) thioacetate] mutilin, was synthesized and structurally characterized by IR, NMR spectra and single-crystal X-ray diffraction. This compound contains a 5-6-8 tricyclic carbon skeleton and a pyrimidine ring. Its crystal is of orthorhombic system, space group P2₁ with a=10.0237(6), b=12.6087(7), c=10.3749(8) Å, β=101.48(1)°, V=1284.99(14) Å³, Z=2, F(000)=540, D_c(Mg/m³)=1.299, µ=0.165 mm^-1, R=0.0649 and wR=0.0797. The in vitro antibacterial activity study using Oxford cup assay showed this compound displayed more potent activity than pleuromutilin and similar antibacterial activity to that of tiamulin.
- pleuromutilin,
- single-crystal structure,
- antibacterial activities
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