Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors.

Sheng C; Xu H; Wang W; Cao Y; Dong G; Wang S; Che X; Ji H; Miao Z; Yao J; Zhang W

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors.

【24h】

Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors.

机译：苯并杂环N-肉豆蔻酰基转移酶抑制剂的等构类似物的设计，合成和抗真菌活性。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

N-myristoyltransferase (NMT) has been a promising new target for the design of novel antifungal agents with new mode of action. A series of benzoxazole and indole derivatives were designed and synthesized as isosteric analogues of benzoheterocyclic NMT Inhibitors. In vitro antifungal assay indicated that the benzoxazole derivatives were far more potent than the indoles. Molecular docking studies revealed that the hydrogen bonding interaction between the benzoheterocyclic core and NMT might be essential in the orientation of the inhibitor to a proper position. The antifungal activity of benzoxazole derivative 8f was comparable or superior to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the benzoheterocyclic NMT inhibitors.

机译：N-肉豆蔻酰基转移酶（NMT）已成为设计具有新作用方式的新型抗真菌剂的有希望的新目标。设计并合成了一系列苯并恶唑和吲哚衍生物，作为苯并杂环NMT抑制剂的等规类似物。体外抗真菌试验表明，苯并恶唑衍生物的效力远高于吲哚。分子对接研究表明，苯并杂环核心与NMT之间的氢键相互作用可能对抑制剂向适当位置的取向至关重要。苯并恶唑衍生物8f的抗真菌活性与氟康唑相当或优于氟康唑，这可以作为进一步研究苯并杂环NMT抑制剂的结构多样性的良好起点。

著录项

来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第9期|共10页
作者
Sheng C; Xu H; Wang W; Cao Y; Dong G; Wang S; Che X; Ji H; Miao Z; Yao J; Zhang W;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词

相似文献

外文文献
中文文献
专利

1. Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors. [J] . Sheng C, Xu H, Wang W, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第9期

机译：苯并杂环N-肉豆蔻酰基转移酶抑制剂的等构类似物的设计，合成和抗真菌活性。
2. Design, synthesis and acaricidal activities of Cyflumetofen analogues based on carbon-silicon isosteric replacement [J] . Zhou Cong, Cheng Jiagao, Beadle Ryan, The Journal of the American Academy of Orthopaedic Surgeons . 2020,第11期

机译：基于碳 - 硅子替代品的Cyflumetofen类似物的设计，合成和Agaricidal活性
3. Design, synthesis and acaricidal activities of Cyflumetofen analogues based on carbon-silicon isosteric replacement [J] . Zhou Cong, Cheng Jiagao, Beadle Ryan, Bioorganic and medicinal chemistry . 2020,第11期

机译：基于碳 - 硅子替代品的Cyflumetofen类似物的设计，合成和Agaricidal活性
4. Design and synthesis of antifungal benzoheterocyclic derivatives by scaffold hopping [C] . Chunquan Sheng, Xiaoying Che, Wenya Wang, International conference of molecular simulations and applied informatics technologies . 2012

机译：支架跳跃法设计和合成抗真菌苯并杂环衍生物
5. Design and synthesis of N-alkoxy analogues of deoxynojirimycin as glycosidase inhibitors. [D] . Sun, Lihong. 1998

机译：设计和合成脱氧野oji霉素的N-烷氧基类似物作为糖苷酶抑制剂。
6. Correction: Sun Y.; et al. Design Synthesis and Evaluation of Novel 2-Hydroxypyrrolobenzodiazepine-511-dione Analogues as Potent Angiotensin Converting Enzyme (ACE) Inhibitors. Molecules 2017 22 1739 [O] . Ying Sun, Yujun Bai, Xirui He, 2018

机译：校正：SunY .;等。设计合成和评估新型2-羟基吡咯并苯并二氮杂511-二酮类似物作为有效的血管紧张素转化酶（ACE）抑制剂。分子2017221739
7. Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes.2. Syntheses and biological activities of 1,4-dialkyl-,1,4-dibenzyl and 1-benzyl-4-alkyl-2-(4',5'-dihydro-1' H-imidazol-2'yl)piperazines and isosteric analogues of imidazoline [O] . Le Bihan, Gaëlle, Rondu, Frédéric, Pele-Tounian, Agnès, 1999

机译：具有II型糖尿病大鼠葡萄糖稳态活性的咪唑啉衍生物的设计与合成2。 1,4-二烷基-，1,4-二苄基和1-苄基-4-烷基-2-（4'，5'-二氢-1'H-咪唑-2'yl）哌嗪的合成及生物活性咪唑啉类似物

Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors.

摘要

著录项

相似文献

相关主题

期刊订阅