当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Sulfamic acid catalyzed synthesis of new 3,5-[(sub)phenyl]-1H-pyrazolebearing N1-isonicotinoyl: and their pharmacological activity evaluation.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-09-19 , DOI: 10.1016/j.bmcl.2020.127558
Jayashri D Bhirud 1 , Rajendra D Patil 1 , Hemant P Narkhede 2
Affiliation  

A sustainable synthesis of new 3,5-[(sub)phenyl]-1H-pyrazole bearing N1-isonicotinoyl derivatives from substituted chalcones and isoniazid by using sulfamic acid and their pharmacological activity evaluation is reported. An anti-oxidant study is performed by using DPPH assay. In vitro anti-mycobacterial activity of compounds bearing R/R′ = 4-CH3/4-F and 3-OCH3/4-Cl showed complete inhibition (99%) at the MIC of 31 and 34 μM respectively. Antibacterial screening of compounds bearing R/R′ = 4-CH3/4-F; 4-OCH3/4-Br; and 4-OCH3/4-Cl has shown noticeable inhibition (27 mm) against Staphylococcus aureus. The anti-cancer bioassay demonstrated that the five compounds were active on human breast cancer cell line MCF-7; however on HeLa cervical cancer cells only two compounds are active in comparison to standard drug Doxorubicin. Higher inhibitory effects observed in this study appear to be dependent on the chloro, bromo, fluoro and methoxy functionality present on the aromatic nucleus. The structures of all the compounds are established using NMR (1H and 13C), FT-IR, Mass and elemental analysis.



中文翻译:

氨基磺酸催化合成新的含3,5-[(亚)苯基] -1H-吡唑的N1-异烟酰胺基:及其药理活性评价。

报道了使用氨基磺酸从取代的查耳酮和异烟肼可持续合成具有N 1-异烟酰酰基衍生物的新型3,5-[(亚)苯基] -1 H-吡唑的合成方法,并对其药理活性进行了评价。通过使用DPPH分析进行抗氧化剂研究。带有R / R'= 4-CH 3 / 4-F和3-OCH 3 / 4-Cl的化合物的体外抗分枝杆菌活性分别在MIC为31和34μM时显示出完全的抑制作用(99%)。对具有R / R'= 4-CH 3 / 4-F的化合物进行抗菌筛选;4-OCH 3 / 4-Br; 和4-OCH 3 / 4-Cl对金黄色葡萄球菌显示出明显的抑制作用(27 mm)。抗癌生物测定结果表明这五种化合物对人乳腺癌细胞MCF-7有活性。然而,与标准药物阿霉素相比,在HeLa子宫颈癌细胞上只有两种化合物具有活性。在这项研究中观察到的更高的抑制作用似乎取决于芳香核上的氯,溴,氟和甲氧基官能团。所有化合物的结构均使用NMR(1 H和13 C),FT-IR,质量和元素分析确定。

更新日期:2020-09-24
down
wechat
bug