Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties | |
Ai, Xin3; Pu, Xiuying1; Yi, Yunpeng3; Liu, Yu3; Xu, Shuijin2; Liang, Jianping3; Shang, Ruofeng3 | |
刊名 | MOLECULES |
2016-11 | |
卷号 | 21期号:11 |
关键词 | pleuromutilin derivatives synthesis antibacterial activity inhibition CYP3A4 |
ISSN号 | 1420-3049 |
DOI | 10.3390/molecules21111488 |
英文摘要 | A series of novel pleuromutilin derivatives with substituted benzimidazole moieties were designed and synthesized from pleuromutilin and 5-amino-2-mercaptobenzimidazole through sequential reactions. All the newly synthesized compounds were characterized by IR, NMR, and HRMS. Each of the derivatives was evaluated in vitro for their antibacterial activity against Escherichia coli (E. coli) and five Gram (+) inoculums. 14-O-((5-amino-benzimidazole-2-yl)thioacetyl)mutilin (3) was the most active compound and showed highest antibacterial activities. Furthermore, we evaluated the inhibition activities of compound 3 on short-term S. aureus and MRSA growth and cytochrome P450 (CYP). The bioassay results indicate that compound 3 could be considered potential antibacterial agents but with intermediate inhibition of CYP3A4. |
资助项目 | Agricultural Science and Technology Innovation Program (ASTIP)[CAAS-ASTIP-2014-LIHPS-04] |
WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
语种 | 英语 |
出版者 | MDPI AG |
WOS记录号 | WOS:000389918200070 |
状态 | 已发表 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.223/handle/2XXMBERH/33561] |
专题 | 生命科学与工程学院 |
通讯作者 | Shang, Ruofeng |
作者单位 | 1.Lanzhou Univ Technol, Coll Life Sci & Engn, 287 Langongping Rd, Lanzhou 730050, Peoples R China 2.Yancheng Shunbao Chem Co Ltd, Yancheng 224555, Peoples R China 3.Lanzhou Inst Husb & Pharmaceut Sci CAAS, Minist Agr, Key Lab Vet Pharmaceut Dev, Key Lab New Anim Drug Project Gansu Prov, 335 Jiangouyan, Lanzhou 730050, Peoples R China |
推荐引用方式 GB/T 7714 | Ai, Xin,Pu, Xiuying,Yi, Yunpeng,et al. Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties[J]. MOLECULES,2016,21(11). |
APA | Ai, Xin.,Pu, Xiuying.,Yi, Yunpeng.,Liu, Yu.,Xu, Shuijin.,...&Shang, Ruofeng.(2016).Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties.MOLECULES,21(11). |
MLA | Ai, Xin,et al."Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties".MOLECULES 21.11(2016). |
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