Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties

doi:10.3390/molecules21111488

	Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties
	Ai, Xin 1; Pu, Xiuying 3; Yi, Yunpeng 1; Liu, Yu 1; Xu, Shuijin 2; Liang, Jianping 1; Shang, Ruofeng 1
刊名	MOLECULES
	2016-11-01
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.
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	MDPI AG
WOS记录号	WOS:000389918200070
内容类型	期刊论文
源URL	[http://ir.lut.edu.cn/handle/2XXMBERH/155449]
专题	生命科学与工程学院
作者单位	1.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; 2.Yancheng Shunbao Chem Co Ltd, Yancheng 224555, Peoples R China 3.Lanzhou Univ Technol, Coll Life Sci & Engn, 287 Langongping Rd, 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).