Benzothiozinone derivatives with anti-tubercular Activity-Further side chain investigation
文献类型：期刊论文
| 作者 | Wu, Xiaomei5; Wang, Wenxin6; Stelitano, Giovanni7; Riabova, Olga4; Wang, Bin3; Niu, Wei2; Cocorullo, Mario7; Shi, Rui5; Chiarelli, Laurent R.7; Makarov, Vadim4 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2024-01-15 |
| 卷号 | 264页码:11 |
| ISSN号 | 0223-5234 |
| 关键词 | Anti -tubercular activity DprE1 inhibitor Benzothiazinone derivatives Structure activity relationship |
| DOI | 10.1016/j.ejmech.2023.115976 |
| 通讯作者 | Lu, Yu(luyu4876@hotmail.com) ; Li, Chuan(chli@simm.ac.cn) ; Qiao, Chunhua(qiaochunhua@suda.edu.cn) |
| 英文摘要 | A series of novel benzothiozinone (BTZ) derivatives were designed, prepared and evaluated for antituberculosis activity. Specifically, the BTZ pharmacophore is retained and the previous heterocyclic ring linker is replaced by alkynyl or vinyl linker, the resulting compounds displayed about 5-fold improved antimycobacterial activity. We further revealed that the linker attached tail group affects the compound metabolic stability, potency and other drug like properties. This work led to the discovery of two compounds (A1 and A11) with acceptable low MICs and improved metabolic stability. The representative compound A11 demonstrated bactericidal efficacy in an acute TB infection mouse model. |
| WOS关键词 | KILL MYCOBACTERIUM-TUBERCULOSIS |
| 资助项目 | Priority Academic Program Development of the Jiangsu Higher Education Institutes (PAPD) |
| 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:001128150100001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/308368]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Lu, Yu; Li, Chuan; Qiao, Chunhua |
| 作者单位 | 1.Zhongshan Inst Drug Discovery, Zhongshan 528400, Guangdong, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Capital Med Univ, Beijing Chest Hosp, Beijing TB & Thorac Tumor Res Inst, Dept Pharmacol,Beijing Key Lab Drug Resistance TB, Beijing 101149, Peoples R China 4.Russian Acad Sci, Res Ctr Biotechnol, Moscow 119071, Russia 5.Soochow Univ, Coll Pharmaceut Sci, MOE Key Lab Geriatr Dis & Immunol, Suzhou Med Coll, Suzhou 215123, Jiangsu, Peoples R China 6.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Jiangsu, Peoples R China 7.Univ Pavia, Dept Biol & Biotechnol, I-27100 Pavia, Italy |
| 推荐引用方式 GB/T 7714 | Wu, Xiaomei,Wang, Wenxin,Stelitano, Giovanni,et al. Benzothiozinone derivatives with anti-tubercular Activity-Further side chain investigation[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,264:11. |
| APA | Wu, Xiaomei.,Wang, Wenxin.,Stelitano, Giovanni.,Riabova, Olga.,Wang, Bin.,...&Qiao, Chunhua.(2024).Benzothiozinone derivatives with anti-tubercular Activity-Further side chain investigation.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,264,11. |
| MLA | Wu, Xiaomei,et al."Benzothiozinone derivatives with anti-tubercular Activity-Further side chain investigation".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 264(2024):11. |
入库方式： OAI收割
来源：上海药物研究所
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