Synthesis,antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyrido

来源 :2015年全国药物化学学术会议暨第五届中英药物化学学术会议 | 被引量 : 0次 | 上传用户：KANTB

【摘要】

：

【作者】

：

Rui Zhang Ju Huang Mingliang Liu

【机构】

：

Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences and Peking Union Medical Co

【出处】

：

2015年全国药物化学学术会议暨第五届中英药物化学学术会议

【发表日期】

：

2015年3期

【关键词】

：

fluoroquinolone derivatives synthesis antimycobacterial activity antibacterial a

下载到本地 , 更方便阅读

下载此文赞助VIP

声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架

论文部分内容阅读

　　A series of novel 1-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives 21-24 containing an oxime-functionalized pyrrolidine moeity were designed,synthesized and evaluated for their biological activity.[1] Our results reveal that compounds 21a,21e and 21j show excellent activity against MTB H37Rv ATCC 27294(MICs: <0.25 μg/mL)and MDR-MTB 6133(MICs: 0.03-0.054 μg/mL).

其他文献

CPUY201112,a novel synthetic small-molecule compound as inhibitor of heat shock protein Hsp90,induce

Heat shock protein 90(Hsp90)is highly expressed in many tumor cells and is associated with the maintenance of malignant phenotypes.Targeting Hsp90 has shown some therapeutic success in solid and hemat

会议

Design,Synthesis and Biological Evaluation of Nitric oxide/Hydrogen Sulfide-Donating Hybrids of 3-n-

会议

Discovery of novel 4,5,6-trisubstituted pyrimidines as covalent BTK inhibitors

Brutions tyrosine kinase(BTK)is a key component of the B-cell receptor signaling pathway which plays a critical role in B-cell development.Ample evidence indicates that the dysregulation of BTK is ass

会议

B-cell malignancyB-cell receptorBTKcovalent drugpyrimidine

钩吻素子抗肿瘤作用靶点的研究

钩吻(Gelsemium elegans Benth.)为马钱科(Loganiaceae)胡蔓藤属(Gelsemium)植物.钩吻全草有毒，民间一直以外用为主，治疗皮肤病.吲哚类生物碱钩吻素子是其主要化学成分，钩吻素子具有良好的抗肿瘤作用，但其作用机制尚不明确[1-3].

会议

钩吻素子抗肿瘤作用靶点HSP90

Design,synthesis and biological activity of polyphenolsbenzohydrazide analogues as sphingosine kinas

The design,synthesis,and biological activity evaluation of the potency of new inhibitors of sphingosine kinases 1 and 2(SphK1 and SphK2),the enzyme that catalyzes the phosphorylation of D-erythro-sphi

会议

sphingosine kinasesstructure-activity relationship

Identification of Nitric Oxide-Releasing Derivatives of Oleanolic Acid as Potential Anti-Colon Cance

The overexpressed GSTπ isozyme in tumor cells was regarded as targets for the design of anti-cancer agents.Herein,a group of GSTπ-based nitric oxide(NO)-releasing derivatives of oleanolic acid(OA)(1–9

会议

Anti-Colonic CancerNitric Oxide donoroleanolic acidWnt/β-catenin pathway

A novel method for synthesis of Lorcaserin Hydrochloride

Lorcaserin was approved in June 2012 by the FDA for the treatment of obesity.1 Several methods for the synthesis of lorcaserin have been reported,but these methods are unsuitable for industrial-scale

会议

lorcaserinsynthesisanti-obesity drug

二硫代硫酮类硫化氢供体化合物的研究进展

硫化氢(hydrogen sulfide,H2S)作为新型的气体信号分子,广泛参与人体生理和病理过程,尤其在高血压、肺动脉高压、帕金森、阿尔兹海默等疾病的发病过程中发挥着重要作用.H2S供体可用来模拟体内H2S的释放过程,对H2S气体的活性研究至关重要,也是潜在的治疗型药物.

会议

H2SH2S供体二硫代硫醇神经保护

基于虚拟筛选的新型PTP1B抑制剂的发现

蛋白酪氨酸磷酸酯酶1B(protein tyrosine phosphatase 1B,PTP1B)在胰岛素和瘦素信号通路中起着重要的双重负调控作用,是治疗2型糖尿病及其综合征的潜在靶标。虽然PTP1B抑制剂的研究成为热点,但是至今没有成功上市的药物。

会议

2型糖尿病蛋白酪氨酸磷酸脂酶1B抑制剂虚拟筛选药效团模型分子对接

Identification of new xanthine oxidase inhibitors by predictive pharmacophore-based virtual screenin

Gout is a heterogeneous disease associated with hyperuricemia and is featured by urate crystals deposited in joints and soft tissues.Xanthine oxidase(XO)is a key enzyme involved in the occurrence of g

会议

xanthine oxidase inhibitorspharmacophorevirtual screening

Synthesis,antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyrido

与本文相关的学术论文