Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus

Karad Sharad C.; Purohit Vishal B.; Raval Dipak K.; Kalaria Piyush N.; Avalani Jemin R.; Thakor Parth; Thakkar Vasudev R.

首页> 外文期刊>RSC Advances >Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus

【24h】

Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus

机译：含有氟化5-芳氧基吡唑核的多羟基喹啉衍生物的绿色合成及药理筛查

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

A novel series of polyhydroquinoline scaffolds 8a-p has been designed and synthesized under ultrasonic irradiation by a one-pot three-component cyclocondensation reaction of 3-methyl-5substituted aryloxy-1-phenyl-1H-pyrazole-4-carbaldehydes 3a-d with malononitrile 7 and various enhydrazinoketones 6a-e in the presence of piperidine as basic catalyst. All the synthesized compounds have been characterized by various spectroscopic techniques and elemental analysis. All the synthesized compounds were evaluated for their in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain and also for their in vitro antimalarial activity against Plasmodium falciparum. Compounds 8c, 8i, 8j, 8l and 8m exhibited excellent antimalarial potency. The cytotoxicity of the synthesized compounds was tested using a bioassay of S. pombe cells at the cellular level. Compounds 8i, 8j, 8k and 8l were found to have maximum toxicity, while compounds 8e, 8m, 8c were found to be less cytotoxic. Some of them displayed luminous antibacterial activity and reasonable antituberculosis activity as compared with the first line drugs.

机译：通过3-甲基-5 - 5取代的芳基氧基-1-苯基-1H-吡唑-4- Carbaldehys 3A-D的单罐三分 - 三分环致反应，设计和合成了一种新的多羟基喹啉支架8A-P的多羟基喹啉支架8A-P。在哌啶作为碱性催化剂存在下，亚锰腈7和各种增强肼基酮6A-E。所有合成的化合物的特征在于各种光谱技术和元素分析。评价所有合成的化合物对其对细菌和真菌的致病菌株组的体外抗菌活性，对抗结核分枝杆菌H37RV菌株的体外抗细胞活性，以及对疟原虫的体外抗疟疾活性。化合物8C，8I，8J，8L和8M表现出优异的抗疟性效力。在细胞水平下使用S.Pombe细胞的生物测定来测试合成化合物的细胞毒性。发现化合物8i，8j，8k和8L具有最大毒性，而发现化合物8e，8m，8c的细胞毒性较少。与第一线药物相比，其中一些显示出明亮的抗菌活性和合理的抗尿嘧啶活性。

著录项

来源
《RSC Advances》 |2015年第21期|共10页
作者
Karad Sharad C.; Purohit Vishal B.; Raval Dipak K.; Kalaria Piyush N.; Avalani Jemin R.; Thakor Parth; Thakkar Vasudev R.;
展开▼
作者单位

Sardar Patel Univ Dept Chem Vallabh Vidyanagar 388120 Gujarat India;

Sardar Patel Univ Dept Chem Vallabh Vidyanagar 388120 Gujarat India;

Sardar Patel Univ Dept Chem Vallabh Vidyanagar 388120 Gujarat India;

Sardar Patel Univ Dept Chem Vallabh Vidyanagar 388120 Gujarat India;

Sardar Patel Univ Dept Chem Vallabh Vidyanagar 388120 Gujarat India;

Sardar Patel Univ BR Doshi Sch Biosci Vallabh Vidyanagar 388120 Gujarat India;

Sardar Patel Univ BR Doshi Sch Biosci Vallabh Vidyanagar 388120 Gujarat India;

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类化学;
关键词

相似文献

外文文献
中文文献
专利

1. Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus [J] . Karad Sharad C., Purohit Vishal B., Raval Dipak K., RSC Advances . 2015,第21期

机译：含有氟化5-芳氧基吡唑核的多羟基喹啉衍生物的绿色合成及药理筛查
2. Synthesis of N-substituted acetamide derivatives of azinane-bearing 1,3,4-oxadiazole nucleus and screening for antibacterial activity [J] . J Iqbal, Aziz-ur-Rehman ., M A Abbasi, Tropical Journal of Pharmaceutical Research . 2017,第2期

机译：含氮杂1,3,4-恶二唑核的N-取代乙酰胺衍生物的合成及抗菌活性的筛选
3. Microwave-assisted synthesis and antimicrobial screening of new imidazole derivatives bearing 4-thiazolidinone nucleus [J] . N. C. Desai, V. V. Joshi, K. M. Rajpara, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2013,第4期

机译：带有4-噻唑烷酮核的新咪唑衍生物的微波辅助合成和抗菌筛选
4. Synthesis and Acetyl Cholinesterase Inhibitory Activity of New Oxazole, 1, 2, 4 - Triazole Derivatives Bearing Carbamazepine as Nucleus [C] . Amjad Gali Eliwi, Zainab Zuhair Mohammad Ali, Fouad A. AL-Saady, International Conference on Materials Engineering and Science . 2020

机译：新氧唑，1,2,4 - 三唑衍生物的合成和乙酰胆碱酯酶抑制活性携带尸毒葡萄球菌
5. New developments toward the synthesis of heterocycles and applications in green chemistry. I. A simple and essentially one-pot synthesis of N-aminated heterocycles using phase transfer catalyst (Aliquat-336). II. Synthesis of pharmaceutically important pyrrole derivatives. III. Applications in green chemistry: Surfactant-mediated environmentally friendly cleavage of aromatic esters and trans-esterification under solvent-free neutral conditions . [D] . Patel, Nitinchandra. 2005

机译：杂环合成的新进展及其在绿色化学中的应用。 I.使用相转移催化剂（Aliquat-336）简单且基本上一锅合成N-胺化的杂环。二。药学上重要的吡咯衍生物的合成。三，在绿色化学中的应用：在无溶剂的中性条件下，表面活性剂介导的环境友好的芳族酯裂解和酯交换反应。
6. Synthesis and Pharmacological In Vitro Investigations of Novel Shikonin Derivatives with a Special Focus on Cyclopropane Bearing Derivatives [O] . Nadine Kretschmer, Antje Hufner, Christin Durchschein, 2021

机译：新型世代素衍生物的合成及药理体外研究特别关注环丙烷轴承衍生物
7. Synthesis of N-substituted acetamide derivatives of azinane-bearing 1,3,4-oxadiazole nucleus and screening for antibacterial activity [O] . Kashif Iqbal, Qaiser Jamal, Javeid Iqbal, 2017

机译：含氮醌1,3,4-二唑核的N-取代的乙酰胺衍生物的合成及抗菌活性筛选
8. Perfluorinated and Partially-Fluorinated Silane Derivatives of Perfluorooctyne: Synthesis Characterization and Chemical Reactivity [R] . Vij, V., Haddad, T. S., Mabry, J. M. 2011

机译：全氟辛烷的全氟化和部分氟化硅烷衍生物：合成表征和化学反应性

Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus

摘要

著录项

相似文献

相关主题

期刊订阅