Design, synthesis, and biological evaluations of substituted pyrazoles as pyrrolomycin analogues against staphylococcal biofilm & nbsp;
文献类型：期刊论文
| 作者 | Huan, Xiang2,3; Wang, Yanhui1,2; Peng, Xiaofeng1,2; Xie, Shanshan1,2; He, Qian2 ; Zhang, Xiaofei2; Lan, Lefu1,2; Yang, Chunhao1,2,3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2022-06-05 |
| 卷号 | 236页码:13 |
| ISSN号 | 0223-5234 |
| 关键词 | Pyrrolomycin analogues Antibacterial agents Gram-positive drug-resistant bacteria Staphylococcal biofilm Substituted pyrazoles |
| DOI | 10.1016/j.ejmech.2022.114309 |
| 通讯作者 | Zhang, Xiaofei(xiaofeizhang@simm.ac.cn) ; Lan, Lefu(llan@simm.ac.cn) ; Yang, Chunhao(chyang@simm.ac.cn) |
| 英文摘要 | The formation of biofilm enables Staphylococcus aureus to resist antibiotics and causes chronic infections. Several compounds of pyrrolomycins are potent antibacterial agents which display inhibition upon staphylococcal biofilms. We designed and synthesized two series of substituted pyrazoles as pyrrolo-mycin analogues. Compounds 17a, 17d and 17h displayed potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA), and 17d showed the most potent activity against MRSA (MIC = 0.0625 mu g/mL), vancomycin-intermediate Staphylococcus aureus (VISA) (MIC = 0.0313 mu g/mL). Further study indicated that compound 17h could significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. In vitro liver microsomal stability was also evaluated and the results manifested that 17h was metabolically stable in human liver microsomes. (C)& nbsp; 2022 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | ANTIBACTERIAL ; ANTIBIOTICS ; RESISTANCE ; DISCOVERY ; AGENT |
| 资助项目 | National Natural Science Foundation of China (NSFC)[21907104] ; National Natural Science Foundation of China (NSFC)[31870127] ; Science and Technology Commission of Shanghai Municipality[19JC1416400] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| WOS记录号 | WOS:000793420300004 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/301101]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhang, Xiaofei; Lan, Lefu; Yang, Chunhao |
| 作者单位 | 1.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210046, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 |
Huan, Xiang,Wang, Yanhui,Peng, Xiaofeng,et al. Design, synthesis, and biological evaluations of substituted pyrazoles as pyrrolomycin analogues against staphylococcal biofilm & nbsp; [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2022,236:13. |
| APA |
Huan, Xiang.,Wang, Yanhui.,Peng, Xiaofeng.,Xie, Shanshan.,He, Qian.,...&Yang, Chunhao.(2022). Design, synthesis, and biological evaluations of substituted pyrazoles as pyrrolomycin analogues against staphylococcal biofilm & nbsp; .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,236,13. |
| MLA |
Huan, Xiang,et al." Design, synthesis, and biological evaluations of substituted pyrazoles as pyrrolomycin analogues against staphylococcal biofilm & nbsp; ".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 236(2022):13. |
入库方式： OAI收割
来源：上海药物研究所
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